标签归档：psi

PSI-697(Synonyms: P-Selectin Inhibitor)

发表于由

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。

PSI-697 (Synonyms: P-Selectin Inhibitor) 纯度: 99.70%

PSI-697 是一种口服的 P-selectin 抑制剂，IC50 值为 125 μM。

PSI-697(Synonyms: P-Selectin Inhibitor)

PSI-697 Chemical Structure

CAS No. : 851546-61-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2832 In-stock
1 mg ￥1400 In-stock
5 mg ￥3500 In-stock
10 mg ￥5000 In-stock
50 mg ￥15000 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PSI-697 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[1].

IC50 & Target

IC50: 125 μM (P-selectin)[1]
体外研究
(In Vitro)

PSI-697 inhibits the binding of a soluble human P-selectin to PSGL-1, in a reproducible concentration-dependent manner inhibiting 50% of binding at a concentration of 125 μM in vitro[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.
体内研究
(In Vivo)

PSI-697 (0-50 mg/kg; p.o.) significantly reduces the number of rolling leukocytes by 39% versus vehicle control[1].
PSI-697 (100 mg/kg; p.o.) reduces thrombus weight by 18% relative to vehicle, without prolonging bleeding time in a rat venous thrombosis model[1].
PSI-697 (30 mg/kg; p.o.; daily; 6 days) promotes thrombus resolution and decreases inflammation in a baboon model of venous thrombosis[2].
PSI-697 ((30 mg/kg; i.g.; daily) decreases vein wall injury in a rat stenosis model of venous thrombosis[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: 4-5 weeks male Sprague-Dawley rat (50-100 g)[1]
Dosage: 0 mg/kg, 30 mg/kg, 50 mg/kg
Administration: Oral administration
Result: At an oral dose of 50 mg/kg reduced the number of rolling leukocytes by 39% versus vehicle control.

Clinical Trial

分子量

367.83

Formula

C21H18ClNO3
CAS 号

851546-61-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 45.8 mg/mL (124.51 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 2.7186 mL 13.5932 mL 27.1865 mL
5 mM 0.5437 mL 2.7186 mL 5.4373 mL
10 mM 0.2719 mL 1.3593 mL 2.7186 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。-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。
参考文献

  • [1]. Bedard PW et al. Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther.

    [2]. Myers DD Jr et al. Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation. Thromb Haemost. 2007 Mar;97(3):400-7.

    [3]. Myers DD Jr et al. Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis. J Vasc Surg. 2006 Sep;44(3):625-32.

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PSI-7409

发表于由

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。

PSI-7409 

PSI-7409是 Sofosbuvir (PSI-7977) 的5′-三磷酸活性代谢物。Sofosbuvir (PSI-7977) 是选择性和高活性的 HCV 核苷酸类似物抑制剂。

PSI-7409

PSI-7409 Chemical Structure

CAS No. : 1015073-42-3

规格 价格 是否有货 数量
1 mg ￥2600 In-stock
5 mg ￥7800 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

PSI-7409 is the active 5′-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.

体外研究
(In Vitro)

PSI-7409 inhibits the enzymatic activities of these NS5BΔ21 polymerases in a dose-dependent manner. The IC50s for PSI-7409 against GT 1b, 2a, 3a, and 4a NS5B polymerases are 1.6 μM, 2.8 μM, 0.7 μM, and 2.6 μM, respectively. PSI-7409 is a weak inhibitor of DNA Pol α (IC50=550 μM). DNA Pol β and γ are not inhibited by 1 mM PSI-7409. A significant amount of RNA product is made in the presence of 500 μM PSI-7409, about 85%[1]. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25 μm over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of ∼100 μM at 4 h and remains at that concentration for 48 h[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.
分子量

500.16

Formula

C10H16FN2O14P3
CAS 号

1015073-42-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 50 mg/mL (99.97 mM; Need ultrasonic)

DMF : < 1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9994 mL 9.9968 mL 19.9936 mL
5 mM 0.3999 mL 1.9994 mL 3.9987 mL
10 mM 0.1999 mL 0.9997 mL 1.9994 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。-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。
参考文献

  • [1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2′-deoxy-2′-fluoro-2′-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96.

    [2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.

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

PSI(Synonyms: Proteasome Inhibitor 1)

发表于由

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。

PSI (Synonyms: Proteasome Inhibitor 1)

PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体 proteasome 抑制剂。PSI 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI具有研究卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的潜力。

PSI(Synonyms: Proteasome Inhibitor 1)

PSI Chemical Structure

CAS No. : 158442-41-2

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

* Please select Quantity before adding items.

生物活性

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].

体外研究
(In Vitro)

PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1].
PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1].
PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1].
PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time: 24 h
Result: Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).

Western Blot Analysis[1]

Cell Line: HBL6 cells
Concentration: 50 nM
Incubation Time: 6 h
Result: Decreased the NF-κB activity by 52%.

分子量

618.76

Formula

C32H50N4O8
CAS 号

158442-41-2
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]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.

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

PSI(Synonyms: Proteasome Inhibitor 1)

发表于由

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。

PSI (Synonyms: Proteasome Inhibitor 1)

PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体 proteasome 抑制剂。PSI 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI具有研究卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的潜力。

PSI(Synonyms: Proteasome Inhibitor 1)

PSI Chemical Structure

CAS No. : 158442-41-2

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

* Please select Quantity before adding items.

生物活性

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].

体外研究
(In Vitro)

PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1].
PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1].
PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1].
PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time: 24 h
Result: Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).

Western Blot Analysis[1]

Cell Line: HBL6 cells
Concentration: 50 nM
Incubation Time: 6 h
Result: Decreased the NF-κB activity by 52%.

分子量

618.76

Formula

C32H50N4O8
CAS 号

158442-41-2
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]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.

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

PSI(Synonyms: Proteasome Inhibitor 1)

发表于由

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。

PSI (Synonyms: Proteasome Inhibitor 1)

PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体 proteasome 抑制剂。PSI 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI具有研究卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的潜力。

PSI(Synonyms: Proteasome Inhibitor 1)

PSI Chemical Structure

CAS No. : 158442-41-2

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

* Please select Quantity before adding items.

生物活性

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].

体外研究
(In Vitro)

PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1].
PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1].
PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1].
PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (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 Cytotoxicity Assay[1]

Cell Line: BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time: 24 h
Result: Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).

Western Blot Analysis[1]

Cell Line: HBL6 cells
Concentration: 50 nM
Incubation Time: 6 h
Result: Decreased the NF-κB activity by 52%.

分子量

618.76

Formula

C32H50N4O8
CAS 号

158442-41-2
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]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.

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