Cat. No. 5181
Alternative Name: OPC-41061
Chemical Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-
Biological ActivityPotent 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.
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 / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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 Tolvaptan 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.
Do you know of a great paper that uses Tolvaptan from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: Tolvaptan, supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, Tocris Bioscience, Vasopressin Receptor Antagonist products
Find multiple products by catalog number
New Products in this Area
Negative control for ELA-14 (Cat.No.6293).ELA-14 (human)
Potent apelin (APJ) receptor agonistRetrobradykinin
Reverse analog of BradykininTASP 0390325
Potent and selective V1B receptor antagonist; orally bioavailableML 233
Non-peptide apelin receptor agonist
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.