标签归档：opc

Cilostazol-d4(Synonyms: OPC-13013-d4)

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。

Cilostazol-d4 (Synonyms: OPC-13013-d4)

Cilostazol-d4 是 Cilostazol 氘代物。Cilostazol (OPC 13013) 是有效、选择性的心血管系统中磷酸二酯酶 3 亚型 PDE 3A 的抑制剂，IC50 值为 0.2 μM。

Cilostazol-d4(Synonyms: OPC-13013-d4)

Cilostazol-d4 Chemical Structure

CAS No. : 1215541-47-1

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生物活性

Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

373.49

Formula

C20H23D4N5O2
CAS 号

1215541-47-1
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9.

    [3]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.

    [4]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19.

    [5]. Ye YL,et al. Cilostazol, a phosphodiesterase 3 inhibitor, protects mice against acute and late ischemic brain injuries.Eur J Pharmacol. 2007 Feb 14;557(1):23-31. Epub 2006 Nov 10.

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生物活性分子抑制剂Cilostazol(Synonyms: 西洛他唑; OPC 13013)

发表于由

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Cilostazol (Synonyms: 西洛他唑; OPC 13013) 纯度: 99.91%

Cilostazol (OPC 13013) 是有效、选择性的心血管系统中磷酸二酯酶 3 亚型 PDE 3A 的抑制剂，IC50 值为 0.2 μM。

Cilostazol(Synonyms: 西洛他唑; OPC 13013)

Cilostazol Chemical Structure

CAS No. : 73963-72-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥660 In-stock
50 mg ￥600 In-stock
100 mg ￥900 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].

IC50 & Target

IC50: 0.2 μM ( PDE 3A)[1]
体外研究
(In Vitro)

Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists[2].
Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-dependently, with an IC50 of 15 μM for SIPA, and with a similar IC50 of 12.5 μM for ADP-induced platelet aggregation[2].
Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells[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)

Cilostazol (clinically used doses; p.o.; for 2 weeks) could alleviate CCl4 -induced hepatic fibrogenesis in vivo, presumably due to its direct effect to suppress HSC activation[3].
Cilostazol (intraperitoneal injection; 10 mg/kg; 7 consecutive days after ischemia) attenuates neurological dysfunctions, brain atrophy and infarct volume, and inhibits astrocyte proliferation/glial scar formation and accelerated the angiogenesis in the ischemic boundary zone 7 and 28 days after ischemia[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: Male C57BL/6J mice[3]
Dosage: 0.1% w/w, 0.3% w/w
Administration: Oral administration; fed a normal diet for 2 weeks
Result: Exhibited a lesser fibrotic area than control groups.
Animal Model: Male ICR mice[4]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 7 consecutive days after ischemia
Result: Had an effectve effects for the late injury.

Clinical Trial

分子量

369.46

Formula

C20H27N5O2
CAS 号

73963-72-1
中文名称

西洛他唑
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 : 50 mg/mL (135.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7067 mL 13.5333 mL 27.0665 mL
5 mM 0.5413 mL 2.7067 mL 5.4133 mL
10 mM 0.2707 mL 1.3533 mL 2.7067 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。

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    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (5.41 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 20.0 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
  • 2.

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

    Solubility: ≥ 2 mg/mL (5.41 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.41 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 20.0 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]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.

    [2]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9.

    [3]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19.

    [4]. Ye YL,et al. Cilostazol, a phosphodiesterase 3 inhibitor, protects mice against acute and late ischemic brain injuries.Eur J Pharmacol. 2007 Feb 14;557(1):23-31. Epub 2006 Nov 10.

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Rebamipide(Synonyms: 瑞巴派特; OPC12759; Proamipide)

发表于由

Rebamipide (Synonyms: 瑞巴派特; OPC12759; Proamipide) 纯度: 99.88%

Rebamipide (OPC12759) 是一种粘膜保护剂。Rebamipide 诱导 COX-2 表达，增加 PGE2 水平，且以 COX-2 依赖性方式增强胃粘膜防御。

Rebamipide(Synonyms: 瑞巴派特; OPC12759; Proamipide)

Rebamipide Chemical Structure

CAS No. : 90098-04-7

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥500 In-stock
500 mg ￥400 In-stock
1 g ￥500 In-stock
5 g ￥1620 In-stock
10 g   询价  
50 g   询价  

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生物活性

Rebamipide (OPC12759) is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].

IC50 & Target

COX-2

 

PGE2

 

Clinical Trial

分子量

370.79

Formula

C19H15ClN2O4
CAS 号

90098-04-7
中文名称

瑞巴派特
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 : 50 mg/mL (134.85 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6969 mL 13.4847 mL 26.9694 mL
5 mM 0.5394 mL 2.6969 mL 5.3939 mL
10 mM 0.2697 mL 1.3485 mL 2.6969 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。

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: 2.5 mg/mL (6.74 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.74 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 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.74 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 MCE 网站选购。
参考文献

  • [1]. Sun WH, et al. Induction of cyclooxygenase-2 in rat gastric mucosa by rebamipide, a mucoprotective agent. J Pharmacol Exp Ther. 2000 Nov;295(2):447-52.

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Mozavaptan-d6(Synonyms: OPC-31260-d6)

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。

Mozavaptan-d6 (Synonyms: OPC-31260-d6)

Mozavaptan-d6 (OPC-31260-d6) 是 Mozavaptan 的氘代物。Mozavaptan (OPC-31260) 是一种 benzazepine 衍生物，也是一种有效，选择性，竞争性和口服活性的加压素 V2 受体拮抗剂，IC50 为 14 nM。Mozavaptan 对 V2 受体的选择性比 V1 受体 (IC50 为 1.2 μ

Mozavaptan-d6(Synonyms: OPC-31260-d6)

Mozavaptan-d6 Chemical Structure

CAS No. : 2750534-83-7

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

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生物活性

Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

433.58

Formula

C27H23D6N3O2
CAS 号

2750534-83-7
中文名称

莫扎伐普坦 d6
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

    [3]. Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52.

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Rebamipide-d4(Synonyms: 瑞巴派特 D4; OPC12759-d4; Proamipide-d4)

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。

Rebamipide-d4 (Synonyms: 瑞巴派特 D4; OPC12759-d4; Proamipide-d4)

Rebamipide D4 (OPC12759 D4) 是 Rebamipide 的氘代物。Rebamipide 是一种粘膜保护剂。Rebamipide 诱导 COX-2 表达，增加 PGE2 水平，且以COX-2 依赖性方式增强胃粘膜防御。

Rebamipide-d4(Synonyms: 瑞巴派特 D4; OPC12759-d4; Proamipide-d4)

Rebamipide-d4 Chemical Structure

CAS No. : 1219409-06-9

规格 价格 是否有货
1 mg ￥2200 询问价格 & 货期
5 mg ￥5300 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Rebamipide D4 (OPC12759 D4) is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].

分子量

374.81

Formula

C19H11D4ClN2O4
CAS 号

1219409-06-9
中文名称

瑞巴派特 d4
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]. Sun WH, et al. Induction of cyclooxygenase-2 in rat gastric mucosa by rebamipide, a mucoprotective agent. J Pharmacol Exp Ther. 2000 Nov;295(2):447-52.

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

3,4-Dehydro Cilostazol(Synonyms: OPC-13015)

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。

3,4-Dehydro Cilostazol (Synonyms: OPC-13015) 纯度: 98.01%

3,4-Dehydro Cilostazol (OPC-13015) 是西洛他唑 (Cilostazol; CLZ; HY-17464) 的活性代谢产物。3,4-Dehydro Cilostazol 可用于药代动力学研究。

3,4-Dehydro Cilostazol(Synonyms: OPC-13015)

3,4-Dehydro Cilostazol Chemical Structure

CAS No. : 73963-62-9

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 ￥1430 In-stock
5 mg ￥1300 In-stock
10 mg ￥2450 In-stock
50 mg ￥5400 In-stock
100 mg ￥9200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study[1].

体内研究
(In Vivo)

3,4-Dehydro Cilostazol (OPC-13015; Oral; 1 mg/kg GLZ and 10 mg/kg CLZ) has a T1/2 of 3.94 hours, a Cmax of 1.39 μM and an AUC0-24 of 4.69 μg•h/ml. The plasma concentration time profiles of GLZ, CLZ & its active metabolite DCLZ are traceable up to 24 h, 12 h and 12 h respectively by oral administration at 1 mg/kg dose of GLZ and 10 mg/kg CLZ[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 Model: Male Wistar rats weighing 200 g[1]
Dosage: 1 mg/kg Glipizide (GLZ) and 10 mg/kg Cilostazol (CLZ) (Pharmacokinetic Analysis)
Administration: Oral
Result: Had a T1/2 of 3.94 hours, a Cmax of 1.39 μM and an AUC0-24 of 4.69 μg•h/ml.

分子量

367.44

Formula

C20H25N5O2
CAS 号

73963-62-9
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 : 5 mg/mL (13.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7215 mL 13.6077 mL 27.2153 mL
5 mM 0.5443 mL 2.7215 mL 5.4431 mL
10 mM 0.2722 mL 1.3608 mL 2.7215 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]. T R S Satheeshmanikandan, et al. Liquid Chromatography – Tandem Mass Spectrometry for the Simultaneous Quantitation of Glipizide, Cilostazol and Its Active Metabolite 3, 4-dehydro-cilostazol in Rat Plasma: Application for a Pharmacokinetic Study. Arzneimittelforschung. 2012 Sep;62(9):425-32.

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Mozavaptan(Synonyms: OPC-31260)

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。

Mozavaptan (Synonyms: OPC-31260) 纯度: 99.89%

Mozavaptan (OPC-31260) 是一种 benzazepine 衍生物，也是一种有效，选择性，竞争性和口服活性的加压素 V2 受体拮抗剂，IC50 为 14 nM。Mozavaptan 对 V2 受体的选择性比 V1 受体 (IC50 为 1.2 μM) 高约 85 倍，并且可以在体内拮抗精氨酸加压素的抗利尿作用。Mozavaptan 可用于低钠血症，抗利尿激素不适当综合征 (SIADH) 和充血性心力衰竭的研究。

Mozavaptan(Synonyms: OPC-31260)

Mozavaptan Chemical Structure

CAS No. : 137975-06-5

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 ￥660 In-stock
10 mg ￥600 In-stock
50 mg ￥1800 In-stock
100 mg ￥2600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Mozavaptan 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Diabetes Related Compound Library
  • Endocrinology Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library

生物活性

Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2].

IC50 & Target

IC50: 14 nM (Vasopressin V2 receptor); 1.2 μM (Vasopressin V1 receptor)[1]
体外研究
(In Vitro)

Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively)[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)

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality[1].
Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner[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 Model: Hydrated conscious rats (300-350 g)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Dose-dependently increased urine flow and decreased urine osmolality.

分子量

427.54

Formula

C27H29N3O2
CAS 号

137975-06-5
中文名称

莫扎伐普坦
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 : 6.2 mg/mL (14.50 mM; Need warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3390 mL 11.6948 mL 23.3896 mL
5 mM 0.4678 mL 2.3390 mL 4.6779 mL
10 mM 0.2339 mL 1.1695 mL 2.3390 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]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

    [2]. Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52.

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

Mozavaptan hydrochloride(Synonyms: OPC-31260 hydrochloride)

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。

Mozavaptan hydrochloride (Synonyms: OPC-31260 hydrochloride) 纯度: 98.16%

Mozavaptan hydrochloride (OPC-31260 hydrochloride) 是一种 benzazepine 衍生物，也是一种有效，选择性，竞争性和口服活性的加压素 V2 受体拮抗剂，IC50 为 14 nM。Mozavaptan hydrochloride 对 V2 受体的选择性比 V1 受体 (IC50 为 1.2 μM) 高约 85 倍，并且可以在体内拮抗精氨酸加压素的抗利尿作用。Mozavaptan hydrochloride 可用于低钠血症，抗利尿激素不适当综合征 (SIADH) 和充血性心力衰竭的研究。

Mozavaptan hydrochloride(Synonyms: OPC-31260 hydrochloride)

Mozavaptan hydrochloride Chemical Structure

CAS No. : 138470-70-9

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 ￥660 In-stock
10 mg ￥600 In-stock
50 mg ￥1800 In-stock
100 mg ￥2600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Mozavaptan hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Endocrinology Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Targeted Diversity Library

生物活性

Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2].

IC50 & Target

IC50: 14 nM (Vasopressin V2 receptor); 1.2 μM (Vasopressin V1 receptor)[1]
体外研究
(In Vitro)

Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively)[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)

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality[1].
Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner[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 Model: Hydrated conscious rats (300-350 g)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Dose-dependently increased urine flow and decreased urine osmolality.

分子量

464.00

Formula

C27H30ClN3O2
CAS 号

138470-70-9
中文名称

盐酸莫扎伐普坦
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 : 20.83 mg/mL (44.89 mM; Need ultrasonic)

H2O : 10 mg/mL (21.55 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1552 mL 10.7759 mL 21.5517 mL
5 mM 0.4310 mL 2.1552 mL 4.3103 mL
10 mM 0.2155 mL 1.0776 mL 2.1552 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

    [2]. Yamaguchi K, et al. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52.

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