化合物OPC-51803 T28257

Product Introduction
Bioactivity


英文名: OPC-51803

描述: OPC-51803是一种可口服的非肽加压素（AVP）V（2）受体选择性激动剂，可用于治疗尿失禁和夜尿。

体外活性: OPC-51803 and dDAVP displaced [(3)H]-AVP binding to human V(2)- and V(1a)-receptors with K(i) values of 91.9+/-10.8 nM (n = 6) and 3.12+/-0.38 nM (n = 6) for V(2)-receptors, and 819+/-39 nM (n = 6) and 41.5+/-9.9 nM (n = 6) for V(1a)-receptors, indicating that OPC-51803 was about nine times more selective for V(2)-receptors, similar to the selectivity of dDAVP.[5]OPC-51803 concentration-dependently increased cyclic adenosine 3', 5'-monophosphate (cyclic AMP) production in HeLa cells expressing human V(2)-receptors with an EC(50) value of 189+/-14 nM (n = 6).[5]

体内活性: OPC-51803 shows antidiuretic action in dogs. OPC-51803 (0.03 to 0.3 mg/kg; oral) decreased urine volume and increased urinary osmolality in a dose-dependent manner in water-loaded dogs.[4] OPC-51803 infusions (0.3 and 3 microg x kg(-1) x min(-1); Intravenous ) did not affect renal or systemic hemodynamics in anesthetized dogs.[4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (99.12 mM)


关键字: OPC-51803

相关产品: Fuscoside | Atosiban acetate | Invopressin | Vasopressin Dimer (parallel) (TFA) | Balovaptan | Dp[Tyr(methyl)2,Arg8]-Vasopressin | (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin | Fedovapagon | Felypressin | Argipressin

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途