SR 49059

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2310/10
SR 49059 | CAS No. 150375-75-0 | Vasopressin Receptor Antagonists
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Description: Selective, orally active vasopressin V1A receptor antagonist
Alternative Names: Relcovaptan

Chemical Name: (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide

Purity: ≥99%

Product Details
Citations (6)
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Reviews

Biological Activity

Potent and selective non-peptide vasopressin V1A receptor antagonist; devoid of agonist activity. Displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors. Potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.

Technical Data

M.Wt:
620.5
Formula:
C28H27Cl2N3O7S
Solubility:
Soluble to 30 mM in DMSO
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
150375-75-0

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

  1. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors.
    Serradeil-Le Gal et al.
    J.Clin.Invest., 1993;92:224
  2. Identification of the binding sites of the SR 49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors.
    Tahtaoui et al.
    J.Biol.Chem., 2003;278:40010
  3. Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes.
    Serradeil-Le Gal et al.
    Biochem.Biophys.Res.Comm., 1994;199:353

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