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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
OPC-31260
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
137975-06-5
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥390.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥350.0 |
| 规格： | 10 mg | 产品价格： | ￥550.0 |
| 规格： | 50 mg | 产品价格： | ￥1200.0 |
| 规格： | 100 mg | 产品价格： | ￥1900.0 |
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Mozavaptan
CAS No. : 137975-06-5
MCE 国际站：Mozavaptan
产品活性：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。
研究领域：GPCR/G Protein
作用靶点：Vasopressin Receptor
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).
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.
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