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Mozavaptan

新型竞争性加压素受体拮抗剂,Mozavaptan (OPC31260)是有口服活性的非肽阴道加压素(vasopressin)V2受体拮抗剂，其IC50值为14nM。

目录号: PC10764 纯度: ≥98%

CAS No. :137975-06-5

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中文名称

Mozavaptan

中文别名

莫扎伐普坦;5-(二甲基氨基)-1-[4-(2-甲基苯甲酰胺基)苯甲酰]-2,3,4,5-四氢-1H-苯并氮杂卓;莫扎伐普坦新药技术转让

英文名称

Mozavaptan

英文别名

Mozavaptan;OPC 31260;5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine;Rizatriptan Benzoate;N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methylBenzamide;N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide;: Mozavaptan;(+/-)-5-dimethylamino-1-[4-(2-methylbenzoylamino)-benzoyl]-2,3,4,5-tetrahydro-1H-benzazepin;5-dimethylamino-1-[4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine;Benzamide,N-(4-((5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methyl;Mozavaptan [INN];N-(4-(((5RS)-5-(Dimethylamino)-;N-(4-((5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methylbenzamide;OPC-31260;OPC31260;5-Dimethylamino-1-(4-(2-methylbenzoylamino)benzoyl)-2,3,4,5-tetrahydro-1H-benzazepine;N-(4-(5-(dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)phenyl)-2-methylbenzamide;N-(4-(((5RS)-5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methylbenzamide;C27H29N3O2;5-(Dimethylamino

Cas No.

137975-06-5

分子式

C₂₇H₂₉N₃O₂

分子量

427.54

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

IC50: 14 nM (Vasopressin V₂ receptor); 1.2 μM (Vasopressin V₁ receptor)

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. K_d value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The K_d of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (K_d of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; K_d of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively).

Medlife 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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hydrated conscious rats (300-350 g)
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 6.2 mg/mL (14.50 mM; Need warming)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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