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

Description:	Selective, orally active vasopressin V_1A 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% (HPLC)
Molecular Weight:	620.5

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.

Compound Libraries for SR 49059

SR 49059 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SR 49059

M. Wt	620.5
Formula	C₂₈H₂₇Cl₂N₃O₇S
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	150375-75-0
PubChem ID	60943
InChi Key	CEBYCSRFKCEUSW-NAYZPBBASA-N
Smiles	O=S(C1=CC(OC)=C(OC)C=C1)(N2[C@@H]([C@@](N5CCC[C@H]5[C@@](N)=O)=O)[C@](C4=CC=CC=C4Cl)(O)C3=C2C=CC(Cl)=C3)=O

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	18.61	30

Preparing Stock Solutions for SR 49059

The following data is based on the product molecular weight 620.5.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.3 mM	5.37 mL	26.86 mL	53.72 mL
1.5 mM	1.07 mL	5.37 mL	10.74 mL
3 mM	0.54 mL	2.69 mL	5.37 mL
15 mM	0.11 mL	0.54 mL	1.07 mL

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References for SR 49059

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

Tahtaoui 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 PMID: 12869559
Serradeil-Le Gal Binding of [³H]SR 49059, a potent nonpeptide vasopressin V_1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm.
Serradeil-Le Gal Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V_1a receptors. J.Clin.Invest. 1993 PMID: 8392086