| CAS NO: | 150683-30-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| Cas No. | 150683-30-0 |
| 别名 | 托伐普坦; OPC-41061 |
| 化学名 | N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide |
| Canonical SMILES | CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C |
| 分子式 | C26H25ClN2O3 |
| 分子量 | 448.94 |
| 溶解度 | ≥ 17.8mg/mL in DMSO |
| 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 | Tolvaptan is a selective and oral active antagonist of arginine vasopressin (AVP) V2-receptor with Ki value of 0.43nM [1]. Tolvaptan is a nonpeptide AVP V2-receptor antagonist. It prevents AVP from binding to V2-receptor. In the in vitro binding assay using HeLa cells expressing human AVP receptor subtypes, tolvaptan shows inhibitory activity against V2 and V1a receptors with Ki values of 0.43nM and 12.3nM, respectively. The V1b receptor and 30 other receptors or ion channels are not sensitive to tolvaptan, indicating that tolvaptan is selective to V2-receptor. Tolvaptan also inhibits the production of cAMP induced by AVP with IC50 value of 8nM [1]. In animal models, the tolvaptan induced aquaresis results in increased urine volume and serum sodium. In rat models of acute and chronic hyponatremia, administration of tolvaptan increases plasma sodium levels and decreases the mortality [1]. References: |
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