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Tolvaptan
- OPC 41061- Soluble in DMSO
- MF: C26H25ClN2O3
- MW: 448.94
Description
Tolvaptan (OPC-41061) is a highly potent, orally active and selective antagonist of the vasopressin V2 receptor.
V2 receptor blockade reduces vasopressin-driven water reabsorption in the kidney and is pharmacologically relevant to aquaretic effects. Tolvaptan is useful for studying renal water balance, vasopressin signaling and V2 receptor-dependent disease mechanisms.
Key Features
- Potent and selective vasopressin V2 receptor antagonist
- Orally active aquaretic pharmacology
- Blocks AVP-driven renal water reabsorption pathways
- Reference tool for V2 receptor signaling studies
Applications
- Vasopressin V2 receptor pharmacology
- Renal water-balance research
- Hyponatremia model studies
- Polycystic kidney disease pathway research
More Information
| Parent CAS No. | 150683-30-0 |
|---|---|
| Chemical Name | N-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
| SMILES | N1(C(=O)C2C=CC(NC(=O)C3C(C)=CC=CC=3)=CC=2C)C2C=CC(Cl)=CC=2C(O)CCC1 |
| MFCD | MFCD09838782 |
| InChi | 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) |
| InChiKey | GYHCTFXIZSNGJT-UHFFFAOYSA-N |
| CID | 216237 |
| Short Description | V2 antagonist |
References
- Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.
- T Hirano et al. Effects of the V2-Receptor Antagonist OPC-41061 and the Loop Diuretic Furosemide Alone and in Combination in Rats. JPET 2000, 292(1), 288-294.
- RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.
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