Tolvaptan
Chemical Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Purity: ≥98%
Biological Activity
Tolvaptan is a 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
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.
Background References
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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.
Kondo et al.
Bioorg.Med.Chem., 1999;7:1743 -
Tolvaptan.
Ghali et al.
Nat.Rev.Drug Discov., 2009;8:611 -
Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury.
Aihara et al.
J.Pharmacol.Exp.Ther., 2014;349:258 -
Chronic administration of oral vasopressin type 2 receptor antagonist tolv. exerts both myocardial and renal protective effects in rats with hypertensive heart failure.
Morooka et al.
Circ.Heart.Fail., 2012;5:484
Product Datasheets
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Citation for Tolvaptan
The citations listed below are publications that use Tocris products. Selected citations for Tolvaptan include:
1 Citation: Showing 1 - 1
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Arginine-Vasopressin Receptor Blocker Conivaptan Reduces Brain Edema and Blood-Brain Barrier Disruption after Experimental Stroke in Mice.
Authors: Zeynalov Et al.
Mol Cells 2015;10:e0136121
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