Catalog Number: 5181
Alternate Names: 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
  • M.Wt:
    448.94
  • Formula:
    C26H25ClN2O3
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    150683-30-0
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.
Background References
  1. 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
  2. Tolvaptan.
    Ghali et al.
    Nat.Rev.Drug Discov., 2009;8:611
  3. 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
  4. Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure.
    Morooka et al.
    Circ.Heart.Fail., 2012;5:484
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Tolvaptan include:

1 Citations: Showing 1 - 1

  1. 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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