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抑制剂描述:

产品名称:Mozavaptan

产品别名:见爱必信官网

英文别名:Mozavaptan

靶点:Vasopressin Receptor

CAS:137975-06-5

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Mozavaptan是一种新型,竞争性的vasopressin受体拮抗剂,作用于V1和V2受体,IC50分别为1.2 μM和14 nM。Mozavaptan (OPC-31260)是一种非肽类竞争性AVP抑制剂,作用于V1和V2受体,选择性比为1:25,说明作用于V2受体选择性相对高。 Mozavaptan (OPC-31260) 竞争性抑制AVP结合到V1和V2受体。

溶解性:Ethanol :1 mg/mL (2.33 mM)
DMSO :1 mg/mL (2.33 mM)

体外研究:

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. Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner.

体内研究: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.

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