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.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
If you know of a relevant reference for Tolvaptan, please let us know.
View Related Products by Product Action
Keywords: Tolvaptan potent selective competitive vasopressin receptors antagonists V2 renal cardial protective renoprotective hyponatremia OPC-41061 Vasopressin Receptors
1 Citation for Tolvaptan
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.
Literature in this Area
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.