Batimastat sodium salt(Synonyms: BB-94 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Batimastat sodium salt (Synonyms: BB-94 sodium salt)

Batimastat(BB-94)钠是广谱的基质金属蛋白酶(MMPs)抑制剂,对MMP-1/2/3/7/9的IC50分别为3/4/20/6/4 nM。

Batimastat sodium salt(Synonyms: BB-94 sodium salt)

Batimastat sodium salt Chemical Structure

CAS No. : 130464-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Batimastat sodium salt 的其他形式现货产品:

Batimastat

生物活性

Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

IC50 & Target

IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)[1]

体外研究
(In Vitro)

Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC50 values of 4 nM and 10 nM, respectively. The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM)[2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC50=230 nM)[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels[2]. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200[4]. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064)[5]. Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.62

Formula

C23H30N3NaO4S2

CAS 号

130464-84-5

中文名称

巴马司他纳盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

Animal Administration
[5][6]

Mice[5]
Six-weeks-old female BALB/c mice are used. Mice are treated i.p. with Batimastat (BB-94, 50 mg/kg) 1 h before and 24 h post-infection. Batimastat is suspended at 50 mg/mL in DMSO and stored frozen at -20°C. Prior to use, it is diluted 20-fold in phosphate buffered saline (PBS), and 500 μL are injected into animals. Control mice are injected with 500 μL of 5% DMSO in PBS. Animals are sacrificed 48 h after i.c. challenge.
Rats[6]
Female Sprague-Dawley rats are administered a single physiological dose of E2 (40 μg/kg in a 0.9% NaCl, 0.4% EtOH vehicle) by intraperitoneal (i.p.) injection at the indicated time intervals prior to tissue collection at necropsy. This in vivo dose level of E2 has been shown to induce changes in uterine wet weight, tissue architecture, and gene expression characteristic of estrogen receptor activation. For all other experiments, animals are i.p. administered a single 40 μg/kg bolus of E2 4 h prior to tissue harvest, while control animals receive vehicle only in all studies. Batimastat is administered i.p. at a dose level (40 mg/kg in a 1× PBS, 0.1% Tween-20 vehicle) shown to be effective at inhibiting MMPs in vivo 4 h prior to E2 or saline control.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Batimastat sodium salt(Synonyms: BB-94 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Batimastat sodium salt (Synonyms: BB-94 sodium salt)

Batimastat(BB-94)钠是广谱的基质金属蛋白酶(MMPs)抑制剂,对MMP-1/2/3/7/9的IC50分别为3/4/20/6/4 nM。

Batimastat sodium salt(Synonyms: BB-94 sodium salt)

Batimastat sodium salt Chemical Structure

CAS No. : 130464-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Batimastat sodium salt 的其他形式现货产品:

Batimastat

生物活性

Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

IC50 & Target

IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)[1]

体外研究
(In Vitro)

Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC50 values of 4 nM and 10 nM, respectively. The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM)[2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC50=230 nM)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels[2]. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200[4]. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064)[5]. Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment[6].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.62

Formula

C23H30N3NaO4S2

CAS 号

130464-84-5

中文名称

巴马司他纳盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

Animal Administration
[5][6]

Mice[5]
Six-weeks-old female BALB/c mice are used. Mice are treated i.p. with Batimastat (BB-94, 50 mg/kg) 1 h before and 24 h post-infection. Batimastat is suspended at 50 mg/mL in DMSO and stored frozen at -20°C. Prior to use, it is diluted 20-fold in phosphate buffered saline (PBS), and 500 μL are injected into animals. Control mice are injected with 500 μL of 5% DMSO in PBS. Animals are sacrificed 48 h after i.c. challenge.
Rats[6]
Female Sprague-Dawley rats are administered a single physiological dose of E2 (40 μg/kg in a 0.9% NaCl, 0.4% EtOH vehicle) by intraperitoneal (i.p.) injection at the indicated time intervals prior to tissue collection at necropsy. This in vivo dose level of E2 has been shown to induce changes in uterine wet weight, tissue architecture, and gene expression characteristic of estrogen receptor activation. For all other experiments, animals are i.p. administered a single 40 μg/kg bolus of E2 4 h prior to tissue harvest, while control animals receive vehicle only in all studies. Batimastat is administered i.p. at a dose level (40 mg/kg in a 1× PBS, 0.1% Tween-20 vehicle) shown to be effective at inhibiting MMPs in vivo 4 h prior to E2 or saline control.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Batimastat sodium salt(Synonyms: BB-94 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Batimastat sodium salt (Synonyms: BB-94 sodium salt)

Batimastat(BB-94)钠是广谱的基质金属蛋白酶(MMPs)抑制剂,对MMP-1/2/3/7/9的IC50分别为3/4/20/6/4 nM。

Batimastat sodium salt(Synonyms: BB-94 sodium salt)

Batimastat sodium salt Chemical Structure

CAS No. : 130464-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Batimastat sodium salt 的其他形式现货产品:

Batimastat

生物活性

Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

IC50 & Target

IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)[1]

体外研究
(In Vitro)

Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC50 values of 4 nM and 10 nM, respectively. The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM)[2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC50=230 nM)[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels[2]. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200[4]. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064)[5]. Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.62

Formula

C23H30N3NaO4S2

CAS 号

130464-84-5

中文名称

巴马司他纳盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

Animal Administration
[5][6]

Mice[5]
Six-weeks-old female BALB/c mice are used. Mice are treated i.p. with Batimastat (BB-94, 50 mg/kg) 1 h before and 24 h post-infection. Batimastat is suspended at 50 mg/mL in DMSO and stored frozen at -20°C. Prior to use, it is diluted 20-fold in phosphate buffered saline (PBS), and 500 μL are injected into animals. Control mice are injected with 500 μL of 5% DMSO in PBS. Animals are sacrificed 48 h after i.c. challenge.
Rats[6]
Female Sprague-Dawley rats are administered a single physiological dose of E2 (40 μg/kg in a 0.9% NaCl, 0.4% EtOH vehicle) by intraperitoneal (i.p.) injection at the indicated time intervals prior to tissue collection at necropsy. This in vivo dose level of E2 has been shown to induce changes in uterine wet weight, tissue architecture, and gene expression characteristic of estrogen receptor activation. For all other experiments, animals are i.p. administered a single 40 μg/kg bolus of E2 4 h prior to tissue harvest, while control animals receive vehicle only in all studies. Batimastat is administered i.p. at a dose level (40 mg/kg in a 1× PBS, 0.1% Tween-20 vehicle) shown to be effective at inhibiting MMPs in vivo 4 h prior to E2 or saline control.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.

    [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54.

    [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5.

    [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92.

    [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726.

    [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Adapalene sodium salt (Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene (CD271) sodium salt 是第三代合成类视黄醇,局部应用于痤疮。Adapalene sodium salt 是一种有效的 RAR 激动剂,对 RARβRARγRARαAC50 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene sodium salt 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene sodium salt 具有抗肿瘤活性。

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene sodium salt Chemical Structure

CAS No. : 911110-93-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Adapalene sodium salt 的其他形式现货产品:

Adapalene

生物活性

Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]

体外研究
(In Vitro)

Adapalene sodium salt (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively[2].
Adapalene sodium salt (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene sodium salt (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene sodium salt (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene sodium salt (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration: 1-200 μM
Incubation Time: 24 hours
Result: Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis[2]

Cell Line: ES-2 cells
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis[3]

Cell Line: LoVo or DLD1 cells
Concentration: 3, 10, 30 μM
Incubation Time: 6, 12, 24 hours
Result: Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.

体内研究
(In Vivo)

Adapalene sodium salt (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.

Clinical Trial

分子量

434.50

Formula

C28H27NaO3

CAS 号

911110-93-5

中文名称

阿达帕林钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.

    [2]. Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.

    [3]. Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Adapalene sodium salt (Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene (CD271) sodium salt 是第三代合成类视黄醇,局部应用于痤疮。Adapalene sodium salt 是一种有效的 RAR 激动剂,对 RARβRARγRARαAC50 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene sodium salt 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene sodium salt 具有抗肿瘤活性。

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene sodium salt Chemical Structure

CAS No. : 911110-93-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Adapalene sodium salt 的其他形式现货产品:

Adapalene

生物活性

Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]

体外研究
(In Vitro)

Adapalene sodium salt (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively[2].
Adapalene sodium salt (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene sodium salt (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene sodium salt (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene sodium salt (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration: 1-200 μM
Incubation Time: 24 hours
Result: Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis[2]

Cell Line: ES-2 cells
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis[3]

Cell Line: LoVo or DLD1 cells
Concentration: 3, 10, 30 μM
Incubation Time: 6, 12, 24 hours
Result: Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.

体内研究
(In Vivo)

Adapalene sodium salt (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.

Clinical Trial

分子量

434.50

Formula

C28H27NaO3

CAS 号

911110-93-5

中文名称

阿达帕林钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.

    [2]. Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.

    [3]. Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Adapalene sodium salt (Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene (CD271) sodium salt 是第三代合成类视黄醇,局部应用于痤疮。Adapalene sodium salt 是一种有效的 RAR 激动剂,对 RARβRARγRARαAC50 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene sodium salt 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene sodium salt 具有抗肿瘤活性。

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene sodium salt Chemical Structure

CAS No. : 911110-93-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Adapalene sodium salt 的其他形式现货产品:

Adapalene

生物活性

Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]

体外研究
(In Vitro)

Adapalene sodium salt (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively[2].
Adapalene sodium salt (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene sodium salt (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene sodium salt (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene sodium salt (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration: 1-200 μM
Incubation Time: 24 hours
Result: Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis[2]

Cell Line: ES-2 cells
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis[3]

Cell Line: LoVo or DLD1 cells
Concentration: 3, 10, 30 μM
Incubation Time: 6, 12, 24 hours
Result: Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.

体内研究
(In Vivo)

Adapalene sodium salt (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.

Clinical Trial

分子量

434.50

Formula

C28H27NaO3

CAS 号

911110-93-5

中文名称

阿达帕林钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.

    [2]. Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.

    [3]. Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole magnesium salt (Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt Chemical Structure

CAS No. : 1198768-91-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole magnesium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole magnesium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

369.72

Formula

C17H21MgN3O3S

CAS 号

1198768-91-0

中文名称

埃索美拉唑镁盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole magnesium salt (Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt Chemical Structure

CAS No. : 1198768-91-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole magnesium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole magnesium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

369.72

Formula

C17H21MgN3O3S

CAS 号

1198768-91-0

中文名称

埃索美拉唑镁盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole magnesium salt (Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole magnesium salt(Synonyms: (S)-Omeprazole magnesium salt; (-)-Omeprazole magnesium salt)

Esomeprazole magnesium salt Chemical Structure

CAS No. : 1198768-91-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole magnesium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole magnesium salt ((S)-Omeprazole magnesium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole magnesium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

369.72

Formula

C17H21MgN3O3S

CAS 号

1198768-91-0

中文名称

埃索美拉唑镁盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole potassium salt (Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt Chemical Structure

CAS No. : 161796-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole potassium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole potassium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

383.51

Formula

C17H18KN3O3S

CAS 号

161796-84-5

中文名称

埃索美拉唑钾盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole potassium salt (Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt Chemical Structure

CAS No. : 161796-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole potassium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole potassium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

383.51

Formula

C17H18KN3O3S

CAS 号

161796-84-5

中文名称

埃索美拉唑钾盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Esomeprazole potassium salt (Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) 是一种有效的具有口服活性质子泵抑制剂,可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,并可用于胃食管反流疾病的研究。

Esomeprazole potassium salt(Synonyms: (S)-Omeprazole potassium salt; (-)-Omeprazole potassium salt)

Esomeprazole potassium salt Chemical Structure

CAS No. : 161796-84-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Esomeprazole potassium salt 的其他形式现货产品:

Esomeprazole magnesium trihydrate Esomeprazole sodium Esomeprazole magnesium

生物活性

Esomeprazole potassium salt ((S)-Omeprazole potassium salt) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole potassium salt has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].

IC50 & Target

H+, K+-ATPase[1][2]

体外研究
(In Vitro)

Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.

体内研究
(In Vivo)

Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury[2]
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.

Clinical Trial

分子量

383.51

Formula

C17H18KN3O3S

CAS 号

161796-84-5

中文名称

埃索美拉唑钾盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

    [2]. Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

    [3]. Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Paromomycin sulfate salt 硫酸盐

Paromomycin sulfate salt 硫酸盐

粉末,生物制剂,适用于细胞培养,≥98%

有货

Paromomycin sulfate salt 硫酸盐

CAS编号 1263-89-4 | 品牌:Jinpan
Paromomycin sulfate salt

MSDS

质检证书(CoA)

相似产品

  • 分子式 C23H45N5O14·xH2SO4
  • PubChem编号 441375

货号 (SKU) 包装规格 是否现货 价格 数量
P431665-1g 1g 期货 Paromomycin sulfate salt 硫酸盐  
P431665-5g 5g 期货 Paromomycin sulfate salt 硫酸盐  

基本信息

产品名称 Paromomycin sulfate salt 硫酸盐
英文名称 Paromomycin sulfate salt
规格或纯度 粉末,生物制剂,适用于细胞培养,≥98%
生化机理 Paromomycin possesses antileishmanial and antibacterial activities. It is used to cure visceral leishmaniasis (VL) and cutaneous leishmaniasis (CL). This aminocyclitol glycoside is active against gram-negative and gram-positive bacteria. It is also active against E. histolytica , D. fragilis and several cestodes, like Taenia saginata , Taenia solium etc. Paromomycin inhibits the initiation and elongation steps of protein synthesis by binding to 16S ribosomal RNA. Paramomycin binds to the A site, which causes defective polypeptide chains to be produced and leads to cell death.

一般描述

General Description

Chemical structure: aminoglycoside Paromomycin or aminosidine, an aminoglycoside belongs to the class of aminoglycosides. This nonabsorbable antibiotic is found at high level in the lumen of the colon.

Application

Paromomycin sulfate salt has been used as a: reference compound in antileishmanial activity RNA-binding ligand and interacts with aptamer. This interaction prevents the binding (and cutting) of dicer to RNA duplex. Recommended for use in cell culture applications at 100mg/L. Paromomycin sulfate salt has been used as a positive control to compare the purine analog antiviral 2′,3′-dideoxyinosine (ddI).

Other Notes

Keep container tightly closed in a dry and well-ventilated place.Keep in a dry place 1g,5g

General Description

Chemical structure: aminoglycoside Paromomycin or aminosidine, an aminoglycoside belongs to the class of aminoglycosides. This nonabsorbable antibiotic is found at high level in the lumen of the colon.

Application

Paromomycin sulfate salt has been used as a: reference compound in antileishmanial activity RNA-binding ligand and interacts with aptamer. This interaction prevents the binding (and cutting) of dicer to RNA duplex. Recommended for use in cell culture applications at 100mg/L. Paromomycin sulfate salt has been used as a positive control to compare the purine analog antiviral 2′,3′-dideoxyinosine (ddI).

Other Notes

Keep container tightly closed in a dry and well-ventilated place.Keep in a dry place 1g,5g

相关属性

CAS编号 1263-89-4
比旋光度 48° (C=1,H2O)
溶解性 H2O:50mg/mL(在 2-8°C 下储存原液。在 37°C 下稳定 5 天。)
RTECS WK2320000
分子式 C23H45N5O14·xH2SO4
品牌 Jinpan
PubChem CID 441375

Paromomycin sulfate salt 硫酸盐

Paromomycin sulfate salt 硫酸盐

适用于植物细胞培养、生物制剂

有货

Paromomycin sulfate salt 硫酸盐

CAS编号 1263-89-4 | 品牌:Jinpan
Paromomycin sulfate salt

MSDS

质检证书(CoA)

相似产品

  • 分子式 C23H45N5O14·xH2SO4
  • PubChem编号 441375

货号 (SKU) 包装规格 是否现货 价格 数量
P431666-5g 5g 期货 Paromomycin sulfate salt 硫酸盐  
P431666-25g 25g 期货 Paromomycin sulfate salt 硫酸盐  

基本信息

产品名称 Paromomycin sulfate salt 硫酸盐
英文名称 Paromomycin sulfate salt
规格或纯度 适用于植物细胞培养、生物制剂
生化机理 Paromomycin inhibits the initiation and elongation steps of protein synthesis by binding to 16S ribosomal RNA. Paramomycin binds to the A site, which causes defective polypeptide chains to be produced and leads to cell death.

一般描述

General Description

Chemical structure: aminoglycoside

Application

Paromomycin, monomycin, is an aminoglycoside antibiotic used to select genetically transformed plants and plant cells.

Other Notes

Keep container tightly closed in a dry and well-ventilated place

General Description

Chemical structure: aminoglycoside

Application

Paromomycin, monomycin, is an aminoglycoside antibiotic used to select genetically transformed plants and plant cells.

Other Notes

Keep container tightly closed in a dry and well-ventilated place

相关属性

CAS编号 1263-89-4
比旋光度 48° (C=1,H2O)
溶解性 H2O:50mg/mL,清澈至微混浊,无色至微黄色
RTECS WK2320000
分子式 C23H45N5O14·xH2SO4
品牌 Jinpan
PubChem CID 441375

Penicillin G sodium salt 钠盐

Penicillin G sodium salt 钠盐

96.0-102.0%

有货

Penicillin G sodium salt 钠盐

CAS编号 69-57-8 | 品牌:Jinpan
Penicillin G sodium salt

MSDS

质检证书(CoA)

相似产品

  • 分子式 C16H17N2O4SNa
  • 分子量356.37

货号 (SKU) 包装规格 是否现货 价格 数量
P433334-5g 5g 期货 Penicillin G sodium salt 钠盐  
P433334-1g 1g 期货 Penicillin G sodium salt 钠盐  

基本信息

产品名称 Penicillin G sodium salt 钠盐
英文名称 Penicillin G sodium salt
别名 Benzylpenicillin sodium salt 钠盐
英文别名 Benzylpenicillin sodium salt
规格或纯度 96.0-102.0%
运输条件 冰袋运输
生化机理 Mode of Action: Inhibits bacterial cell wall synthesis. Antimicrobial spectrum: Gram-positive bacteria.

一般描述

General Description

Chemical structure: ß-lactam Penicillin G is a narrow spectrum natural antibiotic. It is effective against Streptococcus pneumoniae , groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus.

Application

Penicillin G has been used to study penicillin-binding protein 2, and non-toxigenic Corynebacterium diphtheriae isolated from cases of pharyngitis.

Other Notes

Keep container tightly closed in a dry and well-ventilated place. Product contains Penicillin.

General Description

Chemical structure: ß-lactam Penicillin G is a narrow spectrum natural antibiotic. It is effective against Streptococcus pneumoniae , groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus.

Application

Penicillin G has been used to study penicillin-binding protein 2, and non-toxigenic Corynebacterium diphtheriae isolated from cases of pharyngitis.

Other Notes

Keep container tightly closed in a dry and well-ventilated place. Product contains Penicillin.

相关属性

CAS编号 69-57-8
比旋光度 [α]D 300° (C=2,H2O)
熔点 209-212°C
储存温度 2-8°C储存
密度 1.41
分子量 356.37
分子式 C16H17N2O4SNa
品牌 Jinpan
备注 注意: Solutions should be filter sterilized and stored at Store at 2-8°C for 1 week or at -20°C for more lengthy periods. Solutions are stable at 37°C for 3 days. The sodium salt is soluble in H 2 O at 100 mg/mL.
关联CAS 61-33-6

Penicillin G sodium salt 钠盐

Penicillin G sodium salt 钠盐

粉末,生物制剂,适用于细胞培养

有货

Penicillin G sodium salt 钠盐

CAS编号 69-57-8 | 品牌:Jinpan
Penicillin G sodium salt

MSDS

质检证书(CoA)

相似产品

  • 分子式 C16H17N2O4SNa
  • 分子量356.37

货号 (SKU) 包装规格 是否现货 价格 数量
P433335-25000000Units 25000000Units 期货 Penicillin G sodium salt 钠盐  
P433335-10000000Units 10000000Units 期货 Penicillin G sodium salt 钠盐  
P433335-1000000Units 1000000Units 期货 Penicillin G sodium salt 钠盐  
P433335-100000000Units 100000000Units 期货 Penicillin G sodium salt 钠盐  

基本信息

产品名称 Penicillin G sodium salt 钠盐
英文名称 Penicillin G sodium salt
别名 Benzylpenicillin sodium salt 钠盐
英文别名 Benzylpenicillin sodium salt
规格或纯度 粉末,生物制剂,适用于细胞培养
生化机理 Mode of Action: Inhibits bacterial cell wall synthesis. Antimicrobial spectrum: Gram-positive bacteria.

一般描述

General Description

Chemical structure: ß-lactam

Application

Penicillin G is a narrow spectrum natural antibiotic. It is effective against Streptococcus pneumoniae , groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus. It has been used to study the diagnostic and therapeutic implications of gentamicin-resistant Enterococcus faecalis sequence type 6 with reduced penicillin susceptibility and in cell culture both alone and combined with streptomycin and other antibiotics.

Other Notes

1mu,10mu,25mu,100mu Keep container tightly closed in a dry and well-ventilated place.Product contains Penicillin Keep in a dry place.

General Description

Chemical structure: ß-lactam

Application

Penicillin G is a narrow spectrum natural antibiotic. It is effective against Streptococcus pneumoniae , groups A, B, C and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococcus. It has been used to study the diagnostic and therapeutic implications of gentamicin-resistant Enterococcus faecalis sequence type 6 with reduced penicillin susceptibility and in cell culture both alone and combined with streptomycin and other antibiotics.

Other Notes

1mu,10mu,25mu,100mu Keep container tightly closed in a dry and well-ventilated place.Product contains Penicillin Keep in a dry place.

相关属性

CAS编号 69-57-8
比旋光度 [α]D 300° (C=2,H2O)
熔点 209-212°C
溶解性 H2O:100mg/mL(溶液应过滤除菌并在 2-8°C 下保存 1 周或在 -20°C 下长时间保存。溶液在 37°C 下可稳定保存 3 天。)
密度 1.41
分子量 356.37
分子式 C16H17N2O4SNa
品牌 Jinpan
备注 注意: Solutions should be filter sterilized and stored at 2-8°C for 1 week or at -20°C for more lengthy periods. Solutions are stable at 37°C for 3 days. The sodium salt is soluble in H 2 O at 100 mg/mL.
关联CAS 61-33-6

Nigericin sodium salt(Synonyms: 尼日利亚菌素钠盐)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Nigericin sodium salt (Synonyms: 尼日利亚菌素钠盐) 纯度: ≥98.0%

Nigericin sodium salt 是从吸水链霉菌中得到的一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用,NLRP3 的激动剂。

Nigericin sodium salt(Synonyms: 尼日利亚菌素钠盐)

Nigericin sodium salt Chemical Structure

CAS No. : 28643-80-3

规格 价格 是否有货 数量
5 mg ¥900 In-stock
10 mg ¥1500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Nigericin sodium salt 相关产品

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  • Microbial Metabolite Library

生物活性

Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore, a NLRP3 activator[1].

体外研究
(In Vitro)

Nigericin (0.1 µM) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a dose dependent manner. Nigericin inhibits migration and invasion of H460 lung cancer cells[1]. Nigericin (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higher concentrations. Nigericin (0.1-1 nM) significantly decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and 10 nM[2]. Nigericin exhibits higher toxicity on S18 cells than S26 cells, with IC50 of 2.03±0.55 μM and 4.77±2.35 μM, respectively. Nigericin can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces the migration ability of S18 and HONE-1 cells[3]. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC50 of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ngericin (4 mg/kg, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agent DDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin on CSCs in NPC[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

746.94

Formula

C40H67NaO11

CAS 号

28643-80-3

中文名称

尼日利亚菌素钠盐;尼日利亚菌素钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

Ethanol : ≥ 50 mg/mL (66.94 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3388 mL 6.6940 mL 13.3880 mL
5 mM 0.2678 mL 1.3388 mL 2.6776 mL
10 mM 0.1339 mL 0.6694 mL 1.3388 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 6.25 mg/mL (8.37 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (8.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 2.

    请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.35 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.35 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Yakisich JS, et al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310

    [2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9

    [3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006

    [4]. Zhou HM, et al. Suppression of colorectal cancer metastasis by nigericin through inhibition of epithelial-mesenchymal transition. World J Gastroenterol. 2012 Jun 7;18(21):2640-8

Cell Assay
[1]

For RCCs, cells (appr 2000 cells/well) are plated in 96-well cell-culture microplates and incubated over nigericinht in complete media (CM)-RPMI 1640 supplemented with 5% FBS and 2 mM l-glutamine. Cells are then exposed to the appropriate concentration of drug or vehicle for 72 h. For PPSS, cells (appr 500 cells/well) are plated in 96-well cell-culture microplates incubated over Nigericinht in CM to allow them to adhere and then maintained in serum-free media for 7-8 days and then treated with the appropriate concentration of drug or vehicle for 72 h in SFM. Cell viability for cells growing under RCCs and PPSS are evaluated by the MTT assay. The absorbance of solubilized formazan is read at 570 nm using ELISA (enzyme-linked immunosorbent assay) reader. In all cases, the highest concentration of DMSO is used in the control and this concentration is maintained below 0.001% (v/v). This DMSO concentration does not show any significant antiproliferative effect on the cell line in a short-term assay.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
The S18 cells are injected near the scapula of the nude mice. Nine days after injection, the mice are randomly divided into four groups with six animals each (control, DDP, Nigericin and DDP combined with Nigericin). DDP (2.5 mg/kg) is injected intraperitoneally for five continuous days and nigericin (4 mg/kg) is administrated intraperitoneally every two days. Tumor length and width are measured with a vernier caliper every other day. Tumor volume is calculated using the formula V=0.5×(length×width2). The body weights of the mice are recorded every two days. Mice are humanely euthanized when the tumor volume reach 2000 mm3.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Yakisich JS, et al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310

    [2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9

    [3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006

    [4]. Zhou HM, et al. Suppression of colorectal cancer metastasis by nigericin through inhibition of epithelial-mesenchymal transition. World J Gastroenterol. 2012 Jun 7;18(21):2640-8

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8-Bromo-cAMP sodium salt(Synonyms: 8-Br-Camp sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

8-Bromo-cAMP sodium salt (Synonyms: 8-Br-Camp sodium salt) 纯度: 99.91%

8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) 是一种环 AMP 类似物,是一种环 AMP 依赖性蛋白激酶 (PKA) 激活剂。

8-Bromo-cAMP sodium salt(Synonyms: 8-Br-Camp sodium salt)

8-Bromo-cAMP sodium salt Chemical Structure

CAS No. : 76939-46-3

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥605 In-stock
5 mg ¥550 In-stock
10 mg ¥650 In-stock
25 mg ¥800 In-stock
50 mg ¥1360 In-stock
100 mg ¥2312 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA)[1].

IC50 & Target

PKA[1]

体外研究
(In Vitro)

8-Bromo-cAMP sodium salt is a brominated derivative of cyclic AMP. 8-Bromo-cAMP sodium salt enhances the efficiency of cellular reprogramming. 8-Bromo-cAMP sodium salt improves the reprogramming efficiency of human neonatal foreskin fibroblast (HFF1) cells. 8-Bromo-cAMP sodium salt inhibits proliferation, induce differentiation and apoptosis in a malignant glioma cell line (A-172) and an esophageal cancer cell line (Eca-109)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

430.08

Formula

C10H10BrN5NaO6P

CAS 号

76939-46-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (581.29 mM; Need ultrasonic)

H2O : 100 mg/mL (232.51 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3251 mL 11.6257 mL 23.2515 mL
5 mM 0.4650 mL 2.3251 mL 4.6503 mL
10 mM 0.2325 mL 1.1626 mL 2.3251 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Wang Y, et al. A cyclic AMP analog, 8-Br-cAMP, enhances the induction of pluripotency in human fibroblast cells. Stem Cell Rev. 2011 Jun;7(2):331-41.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Reparixin L-lysine salt(Synonyms: Repertaxin L-lysine salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Reparixin L-lysine salt (Synonyms: Repertaxin L-lysine salt) 纯度: 99.93%

Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。

Reparixin L-lysine salt(Synonyms: Repertaxin L-lysine salt)

Reparixin L-lysine salt Chemical Structure

CAS No. : 266359-93-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1559 In-stock
2 mg ¥990 In-stock
5 mg ¥1650 In-stock
10 mg ¥2750 In-stock
25 mg ¥5500 In-stock
50 mg ¥8500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.

IC50 & Target[1][5]

CXCR1wt

5.6 nM (IC50, in L1.2 cells)

CXCR1Ile43Val

80 nM (IC50, in L1.2 cells)

CXCR1

1 nM (IC50, in cells)

CXCR2

∼100 nM (IC50, in cells)

体外研究
(In Vitro)

Reparixin is a potent functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively)[1]. Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [14C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50 µg/mL, but lower at higher concentrations. Although radioactivity is rapidly distributed into rat tissues, Vss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t1/2~0.5 h) than in dogs (t1/2~10 h)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

429.57

Formula

C20H35N3O5S

CAS 号

266359-93-7

中文名称

瑞帕利辛L-赖氨酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 100 mg/mL (232.79 mM; Need ultrasonic)

DMSO : 100 mg/mL (232.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3279 mL 11.6395 mL 23.2791 mL
5 mM 0.4656 mL 2.3279 mL 4.6558 mL
10 mM 0.2328 mL 1.1640 mL 2.3279 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 40 mg/mL (93.12 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Moriconi A, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002.

    [2]. Bertini R, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54.

    [3]. Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40

    [4]. Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE TREATMENT OF BONE LOSS AND/OR PAIN. US 20170105971 A1.

    [5]. Bertini R, et al. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.

Cell Assay
[1]

L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37°C for 15 min in the presence of vehicle or of Reparixin (1 nM-1 μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber. Different agonists are seeded in the lower compartment of the chamber at the following concentrations: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, 30 nM C5a. The chemotactic chamber is incubated at 37°C in air with 5% CO2 for 45 min (human PMNs) or 2 h (monocytes). At the end of incubation, the filter is removed, fixed, and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding. L1.2 migration is evaluated using 5 μm pore size Transwell filters[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Rats and Dogs[3]
Male and female Sprague-Dawley CD (albino) rats and male Lister Hooded (partially pigmented) rats are used. Male and female beagle Dogs (age about 15 months, bodyweight range 8.3-9.4 kg at the time of dosing) are used. Rats and Dogs are dosed i.v. with repurified [14C]-Reparixin free acid and an equivalent quantity of L-lysine suitably radiodiluted with Reparixin L-lysine salt in a solution of sterile isotonic (0.9%, w/v) saline. Rats are dosed with a solution of total drug concentration 9 mg/mL at a dose volume of 5 mL/kg (30 mg free Reparixin /kg) by bolus injection into a caudal vein. Dogs are dosed with a solution of total drug concentration 100 mg/mL at a dose volume of 0.5 mL/kg (33 mg free Reparixin/kg) by bolus injection into a superficial forelimb vein.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Moriconi A, et al. Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2. J Med Chem. 2007 Aug 23;50(17):3984-4002.

    [2]. Bertini R, et al. Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2non-competitive allosteric inhibitor. Br J Pharmacol. 2012 Jan;165(2):436-54.

    [3]. Midgley I, et al. Species differences in the pharmacokinetics and metabolism of reparixin in rat and dog. Xenobiotica. 2006 May;36(5):419-40

    [4]. Catrina, Anca, et al. METHODS AND COMPOUNDS FOR THE TREATMENT OF BONE LOSS AND/OR PAIN. US 20170105971 A1.

    [5]. Bertini R, et al. Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Etomoxir sodium salt(Synonyms: (R)-(+)-Etomoxir sodium salt)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Etomoxir sodium salt (Synonyms: (R)-(+)-Etomoxir sodium salt) 纯度: ≥98.0%

Etomoxir((R)-(+)-Etomoxir) sodium salt 是肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂,通过抑制 CPT-1a 可抑制脂肪酸氧化,并抑制人、大鼠和豚鼠中棕榈酸酯的氧化。

Etomoxir sodium salt(Synonyms: (R)-(+)-Etomoxir sodium salt)

Etomoxir sodium salt Chemical Structure

CAS No. : 828934-41-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥836 In-stock
5 mg ¥760 In-stock
10 mg ¥1450 In-stock
50 mg ¥5100 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig[1].

IC50 & Target

CPT-1a[2]

体外研究
(In Vitro)

Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells[2].
Etomoxir does not affect the activities of the cardiolipin biosynthetic and remodeling enzymes but causes a reduction in [1-14C]palmitic acid or [1-14C]oleic acid incorporation into cardiolipin[2].
Etomoxir increases [1,3-3H]glycerol incorporation into cardiolipin. The mechanism is a 33% increase in glycerol kinase activity, which produces an increased glycerol flux through the de novo pathway of cardiolipin biosynthesis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Rat heart H9c2 myoblastic cells
Concentration: 1-80 μM
Incubation Time: 2 hours
Result: Reduced the incorporation of [1-14C]fatty acids into CL and PtdGro in H9c2 cardiac myoblast cells but did not affect total incorporation of radioactivity into these cells.

体内研究
(In Vivo)

Etomoxir significantly inhibits the decrease of bone mineral density (BMD) and bone breaking strength in db/db and high fat (HF)-fed mice and suppresses the reduction of BMSCs-differentiated osteoblasts[3].
Etomoxir inhibits the increase of mitochondrial ROS generation in db/db and HF-fed mice and osteoblasts[3].
Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates[4]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 80 male C57BLKS/J lar-Leprdb/db mice[3]
Dosage: 1 mg/kg
Administration: Intraperitoneally injected; twice every week
Result: Serum alkaline phosphatase was increased in db/db mice, which event was significantly suppressed by Etomoxir. Serum level of osteocalcin, a marker of bone formation, was reduced in db/db mice and Etomoxir markedly inhibited the reduction of osteocalcin. Serum tartrate-resistant acid phosphatase was elevated in db/db mice which phenomenon was significantly suppressed by Etomoxir.
Animal Model: Rats[4]
Dosage: 20 mg/kg
Administration: Injected daily; for 8 days
Result: Etomoxir-treated rats displayed a 44% reduced cardiac CPT-I activity.

分子量

320.74

Formula

C15H18ClNaO4

CAS 号

828934-41-4

中文名称

乙莫克舍钠盐;(R)-(+)-乙莫克舍钠盐;(+)-乙莫克舍钠盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (311.78 mM; Need ultrasonic)

H2O : 5 mg/mL (15.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1178 mL 15.5890 mL 31.1779 mL
5 mM 0.6236 mL 3.1178 mL 6.2356 mL
10 mM 0.3118 mL 1.5589 mL 3.1178 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 3.33 mg/mL (10.38 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (7.79 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.79 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.79 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Roddy S O’Connor, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations.Sci Rep. 2018 Apr 19;8(1):6289.

    [2]. Fred Y Xu,et al.Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells.J Lipid Res. 2003 Feb;44(2):415-23.

    [3]. Jun Li, et al. FFA-ROS-P53-mediated mitochondrial apoptosis contributes to reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus.Sci Rep. 2015 Jul 31;5:12724.

    [4]. Joost J F P Luiken, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates.Biochem J. 2009 Apr 15;419(2):447-55.

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