| 货号 | 5181/50 |
| 别名 | N-[4-[(7-Chloro-2,3,4,5-tetrahydro- |
| 供应商 | Tocris |
| 生物活性 | Potent and selective competitive vasopressin V2 receptor antagonist (Ki values are 0.06 and 12.3 nM for V2 and V1a receptors respectively). Decreases urine osmolality and increases serum sodium concentrations. Delays the onset of end-stage renal disease in a mouse model of polycystic kidney disease. Exhibits myocardial and renal protective effects in hypertensive heart failure rats. Orally active. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 448.94 |
| 分子式 | C26H25ClN2O3 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in ethanol |
| 参考文献 | Aiharaet al (2014) Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury. J.Pharmacol.Exp.Ther. 349 258. PMID: 24570071. Morookaet al (2012) Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 5 484. PMID: 22628529. Ghaliet al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611. PMID: 19644472. Kondoet al (1999) 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist. Bioorg.Med.Chem. 7 1743. PMID: 10482466. |