| CAS NO: | 150683-30-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 448.94 |
|---|---|
| Formula | C26H25ClN2O3 |
| CAS No. | 150683-30-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 90 mg/mL (200.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: 6 mg/mL (13.4 mM) | |
| Other info | Chemical Name: N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide InChi Key: GYHCTFXIZSNGJT-XMMPIXPASA-N InChi Code: InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)/t24-/m1/s1 SMILES Code: O=C(NC1=CC=C(C(N2CCC[C@@H](O)C3=CC(Cl)=CC=C32)=O)C(C)=C1)C4=CC=CC=C4C |
| Synonyms | OPC41061; Tolvaptan; OPC 41061; OPC-41061; trade names Samsca; Jinarc; Resodim. |
| In Vitro | In vitro activity: Tolvaptan blocks the binding of [(3)H]AVP to human V(2) receptors with 29-fold greater selectivity than that for V(1a) receptors, and showed no inhibition of V(1b) receptors. Tolvaptan inhibits not only the binding of [(3)H]AVP but also the AVP-induced production of cyclic AMP in human V(2)-receptor-expressing HeLa cells. Tolvaptan shows marked aquaresis in healthy and diseased animals. Tolvaptan causes a concentration-dependent inhibition of arginine vasopressin-induced cAMP production with an apparent IC(50) of 0.1 nM in autosomal dominant polycystic kidney disease (ADPKD) cells. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits AVP-induced Cl(-) secretion and decreases in vitro cyst growth of ADPKD cells cultured within a three-dimensional collagen matrix. |
|---|---|
| In Vivo | Tolvaptan improves hyponatremia, resulting in the prevention of death, and improves organ water retention in rat models with acute and chronic hyponatremia. Tolvaptan reduces cardiac preload without unfavorable effects on renal functions, systemic hemodynamics, or circulating neurohormones in dogs with heart failure (HF). Tolvaptan shows a decrease in kidney weight as well as in cyst and fibrosis volume in animal models of human polycystic kidney disease (PKD). Tolvaptan markedly elevates electrolyte-free water clearance (E-CH(2)O) or aquaresis to a positive value and increases urinary Arginine vasopressin (AVP) excretion in rats with heart failure. |
| Animal model | Rats |
| Formulation & Dosage | N/A |
| References | Cardiovasc Drug Rev. 2007 Spring;25(1):1-13; Biochem Pharmacol. 2008 Mar 15;75(6):1322-30. |
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