SR 49059

Name: SR 49059
Brand: Tocris Bioscience
SKU: 2310

Tocris Bioscience, part of Bio-Techne | Catalog # 2310

Citations (35)

COA / SDS

Selective, orally active vasopressin V1A receptor antagonist

Key Product Details

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%
Molecular Weight:	620.5 kDa

View Full Technical Details for SR 49059

Technical Data
Citations

Biological Activity for SR 49059

SR 49059 is a potent and selective non-peptide vasopressin V_1A receptor antagonist; devoid of agonist activity. Displays high affinity and efficacy at both rat (K_i = 1.6 nM) and human (K_i = 1.1 - 6.3 nM) V_1A 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 for SR 49059

M. Wt	620.5 kDa
Formula	C₂₈H₂₇Cl₂N₃O₇S
Storage	Store at +4°C
Purity	≥99%
CAS Number	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.

Solubility for SR 49059

Solubility

Soluble Soluble to 30 mM in DMSO

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References for SR 49059

References are publications that support the biological activity of the product.

Haam J, Halmos K, Di S, Tasker J Nutritional state-dependent ghrelin activation of vasopressin neurons via retrograde trans-neuronal-glial stimulation of excitatory GABA circuits. J Neurosci, 2014;34(18):6201-13. 2014 PMID: 24790191
Serradeil-Le Gal et al. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V_1a receptors. J.Clin.Invest., 1993;92:224 PMID: 8392086
Tahtaoui et al. Identification of the binding sites of the SR 49059 nonpeptide antagonist into the V_1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors. J.Biol.Chem., 2003;278:40010 PMID: 12869559
Serradeil-Le Gal et al. Binding of [³H]SR 49059, a potent nonpeptide vasopressin V_1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm., 1994;199:353