Mozavaptan hydrochloride|138470-70-9|(OPC-31260 hydrochloride)-陌孚医药/Medlife

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Mozavaptan hydrochloride (Synonyms: OPC-31260 hydrochloride)

目录号: PL11616 纯度: ≥98%

CAS No. :138470-70-9

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中文名称	Mozavaptan hydrochloride
中文别名	莫扎伐普坦盐酸盐;盐酸莫扎伐普坦;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-苯并氮杂卓盐酸盐
英文名称	Mozavaptan hydrochloride
英文别名	Benzamide,N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-,hydrochloride (1:1);Benzamide,N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-...;Mozavaptan (hydrochloride);N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide,hydrochloride;Mozavaptane hydrochloride (JAN);Physuline;UNII-F39AR1YW1O;5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride;Mozavaptan hydrochloride;N-[4-(5-Dimethylamino-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]-2-methylbenzamide hydrochloride;N-[4-[[5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methylbenzamide hydrochloride
Cas No.	138470-70-9
分子式	C₂₇H₂₉N₃O₂^.HCl
分子量	464.00
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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。
生物活性	Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V 2 receptor antagonist with an IC 50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V 2 receptor over V 1 receptor (IC 50 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.
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. 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). 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.

溶解度数据	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

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