Mozavaptan (hydrochloride) (OPC-31260 hydrochloride) 是一种苯并氮杂类衍生物,是一种有效的、选择性的、竞争性的、具有口服活性的加压素 V2 受体拮抗剂,IC50 为 14 nM。
Cas No. | 138470-70-9 |
别名 | 莫扎伐普坦盐酸盐,OPC-31260 hydrochloride |
Canonical SMILES | CC1=C(C(NC2=CC=C(C(N3C(C=CC=C4)=C4C(N(C)C)CCC3)=O)C=C2)=O)C=CC=C1.Cl |
分子式 | C27H29N3O2•HCl |
分子量 | 464 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Mozavaptan is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors located in the liver (V1; IC50 = 1.2 µM) and kidney (V2; IC50 = 14 nM). At 10-100 µg/kg, mozavaptan can inhibit the antidiuretic action of AVP, promoting aquaresis when administered intravenously to rats. The therapeutic potential of mozavaptan in ectopic antidiuretic hormone syndrome, heart failure, and other complications related to hyponatremia has been studied. |