Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mozavaptan (OPC-31260) 是 benzazepine 衍生物,是一种竞争性加压素受体拮抗剂,作用于 V1 和 V2 受体,IC50 分别为 1.2 μM 和 14 nM。它可在体内拮抗精氨酸加压素的抗利尿作用,可用于低钠血症、抗利尿激素不适当综合征和充血性心力衰竭的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 137 | 现货 | ||
5 mg | ¥ 289 | 现货 | ||
10 mg | ¥ 455 | 现货 | ||
25 mg | ¥ 691 | 现货 | ||
50 mg | ¥ 993 | 现货 | ||
100 mg | ¥ 1,570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 322 | 现货 |
产品描述 | Mozavaptan (OPC-31260) is a competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively. |
靶点活性 | V2 receptor:14 nM, Vasopressin receptor 1:1.2 μM |
体外活性 | Mozavaptan (OPC-31260) is a nonpeptide, orally effective competitive inhibitor of AVP with a V2:V1 receptor selectivity ratio of 25:1 indicating relative V2 receptor selectivity. [1] Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner. [2] |
体内活性 | Mozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. OPC-31260 dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats. [2] |
激酶实验 | To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis[1]. |
别名 | 莫扎伐坦, OPC31260l, OPC-31260 |
分子量 | 427.54 |
分子式 | C27H29N3O2 |
CAS No. | 137975-06-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (52.63 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.339 mL | 11.6948 mL | 23.3896 mL | 58.4741 mL |
5 mM | 0.4678 mL | 2.339 mL | 4.6779 mL | 11.6948 mL | |
10 mM | 0.2339 mL | 1.1695 mL | 2.339 mL | 5.8474 mL | |
20 mM | 0.1169 mL | 0.5847 mL | 1.1695 mL | 2.9237 mL | |
50 mM | 0.0468 mL | 0.2339 mL | 0.4678 mL | 1.1695 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Mozavaptan 137975-06-5 GPCR/G Protein Vasopressin Receptor AVP 莫扎伐坦 OPC31260 diuretic OPC31260l hyponatremia Nonpeptide OPC-31260 SIADH OPC 31260 inhibit benzazepine arginine vasopressin-V2 Inhibitor inhibitor