Biological Activity
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.
Compound Libraries
Tolvaptan is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 448.94 |
| Formula | C26H25ClN2O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 150683-30-0 |
| PubChem ID | 216237 |
| InChI Key | GYHCTFXIZSNGJT-UHFFFAOYSA-N |
| Smiles | OC1C2=C(C=CC(Cl)=C2)N(C(C3=C(C)C=C(NC(C4=CC=CC=C4C)=O)C=C3)=O)CCC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.89 | 100 | |
| ethanol | 4.49 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 448.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.23 mL | 11.14 mL | 22.27 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kondo et 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
Ghali et al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611 PMID: 19644472
Aihara et 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
Morooka et 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
Keywords: Tolvaptan, supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, OPC-41061, Vasopressin, Receptors, Vasopressin, Receptors, Tocris Bioscience
