SR 49059A potent and selective AVP Receptor V1a antagonist

SR 49059 (CAS 150375-75-0)

SR 49059 | CAS 150375-75-0 is rated 5.0 out of 5 by 1.
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Synonym: Relcovaptan
Application: A potent and selective AVP Receptor V1a antagonist
CAS Number: 150375-75-0
Purity: ≥99%
Molecular Weight: 620.50
Molecular Formula: C28H27Cl2N3O7S
* Refer to Certificate of Analysis for lot specific data (including water content).
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SR 49059 is a potent, selective, non-peptide, orally active AVP Receptor V1a (Vasopressin V1a) antagonist. Devoid of agonist activity SR 49059 shows 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.


References

Serradeil-Le Gal et al (1993) Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J.Clin.Invest. 92 224. Serradeil-Le Gal et al (1994) Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm. 199 353. Tahtaoui et al (2003) 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. J.Biol.Chem. 278 40010.

Physical State :
Solid
Solubility :
Soluble in DMSO (30 mM).
Storage :
Store at 4° C
Boiling Point :
~868.0° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
Platelet aggregation: IC50 = 3.7 nM (human); AVP Receptor V1a: IC50 = 13 nM (human)
Ki Data :
AVP Receptor V1a: Ki= 0.19 nM (human); V1A receptors: Ki= 1.1-6.3 nM (human); V1A receptors: Ki= 1.6 nM (rat); AVP Receptor V2: Ki= 178 nM (human)
pK Values :
pKa: 10.95 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
nwg
PubChem CID :
60943
MDL Number :
MFCD00922133
SMILES :
COC1=C(C=C(C=C1)S(=O)(=O)N2[C@H]([C@](C3=C2C=CC(=C3)Cl)(C4=CC=CC=C4Cl)O)C(=O)N5CCC[C@H]5C(=O)N)OC

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Cenksoy Cenksoy, C. et al. (PubMed 24405730) presented a potential novel strategy, inhibition of vasopressin-induced VEGF secretion by SR 49059, for decreasing the incidence of ovarian hyperstimulation syndrome in the hyperstimulated rat model. -SCBT Publication Review
Date published: 2015-03-02
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