SR 49059

Cat. No. 2310

SR 49059 C28H27Cl2N3O7S [150375-75-0]

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Alternative Name: 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

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / 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:

Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Acta Neurochir Suppl 34 852. PMID: 24517977.

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.

Manaenko et al (2011) Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice. BMC Neurosci 111 191. PMID: 21725754.

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Keywords: SR 49059, supplier, Selective, orally, active, vasopressin, V1a, receptor, antagonists, V2, Receptors, SR49059, Tocris Bioscience, Vasopressin Receptor Antagonist products

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