Cat. No. 5181

Tolvaptan C26H25ClN2O3 [150683-30-0]

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Alternative Name: OPC-41061

Chemical Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide

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.

Technical Data

Soluble to 100 mM in DMSO and to 10 mM in ethanol
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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.

Ghali et al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611. PMID: 19644472.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Tolvaptan include:

Zeynalov et al (2015) Arginine-Vasopressin Receptor Blocker Conivaptan Reduces Brain Edema and Blood-Brain Barrier Disruption after Experimental Stroke in Mice. Mol Cells 10 e0136121. PMID: 26275173.

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Keywords: Tolvaptan, supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, Tocris Bioscience, Vasopressin Receptor Antagonist products

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