Cat. No. 2310
Alternative Name: Relcovaptan
Chemical Name: (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlo
Biological ActivityPotent 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.
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.
Certificate of Analysis / Safety Data Sheet
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. PMID: 12869559.
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.
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. PMID: 8392086.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for SR 49059 include:
Zhu et al (2013) Arginine vasopressin enhances cell survival via a G protein-coupled receptor kinase 2/β-arrestin1/extracellular-regulated kinase 1/2-dependent pathway in H9c2 cells. Mol Pharmacol 84 227. PMID: 23690069.
Do you know of a great paper that uses SR 49059 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: SR 49059, supplier, Selective, orally, active, vasopressin, V1a, receptor, antagonists, V2, Receptors, SR49059, Tocris Bioscience, Vasopressin Receptor Antagonist products
Find multiple products by catalog number
New Products in this Area
Potent human MC1 receptor antagonist; also MC3 and MC5 partial agonistNeuropeptide S (Mouse)
Potent endogenous neuropeptide S receptor (NPSR) agonistML 382
MrgX1 (SNSR4) positive allosteric modulatorK-(D-1-Nal)-FwLL-NH2
High affinity and potent ghrelin receptor inverse agonistNeuropeptide S (Rat)
Potent endogenous neuropeptide S receptor agonistNeuropeptide S (human)
Potent endogenous neuropeptide S receptor agonist
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.