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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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 the degree 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|
References are publications that support the biological activity of the product.
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 tolv. exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 5 484 PMID: 22628529
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Keywords: Tolvaptan, Tolvaptan supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, OPC-41061, Vasopressin, Receptors, 5181, Tocris Bioscience
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
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Literature in this Area
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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.