Tolvaptan

Key Product Details

Product Description

Tolvaptan is a potent and selective competitive vasopressin V₂ receptor antagonist (K_i values are 0.06 and 12.3 nM for V₂ and V_1a 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.

Product Specifications for Tolvaptan

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Tolvaptan

The following data is based on the product molecular weight 448.94.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 6 publications citing the usage of this product.

• Morooka Chronic administration of oral vasopressin type 2 receptor antagonist tolv. exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 2012 PMID: 22628529
• Ghali Tolvaptan. Nat.Rev.Drug Discov. 2009 PMID: 19644472
• Aihara 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. 2014 PMID: 24570071
• Kondo 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. 1999 PMID: 10482466

Product Documents for Tolvaptan