150375-75-0

150375-75-0 structure

Name: SR 49059
Chemical Name: SR 49059,(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
CAS Number: 150375-75-0
Molecular Formula: C₂₈H₂₇Cl₂N₃O₇S
Molecular Weight: 620.50
Catalog: Signaling Pathways GPCR/G Protein Vasopressin Receptor
Create Date: 2018-12-24 22:19:58
Modify Date: 2024-01-02 12:03:27
SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].

Name	SR 49059,(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
Synonyms	reclovaptan cis-Ned 19 INDOL-2-YLCARBONYL)-L-PROLINAMIDE Relcovaptan SR 49059

Description	SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor
Target	Ki: 1.4±0.3 nM (vasopressin V1a)[1].
In Vivo	SR 49059 (SR-49059) (2 mg/kg and 30 mg/kg; i.p.; once) shows neuroprotective effects in ischemic brain injury when injected early after occlusion of the middle cerebral artery (MCA)[2]. Animal Model: Male Wistar rats, weighing 300 to 350 g, cerebral focal ischemia model[2] Dosage: 2 mg/kg and 30 mg/kg dissolved in 10% dimethyl sulfoxide Administration: Intraperitoneal injection, once Result: Significantly reduced infarction volume measured at 48 hours after the arterial occlusion. Reduced neurological deficits and ischemic brain edema.
References	[1]. Serradeil-Le Gal C, et al. Effect of SR-49059, a vasopressin V1a antagonist, on human vascular smooth muscle cells. Am J Physiol. 1995 Jan;268(1 Pt 2):H404-10. [2]. Shuaib A, et al. Effects of nonpeptide V(1) vasopressin receptor antagonist SR-49059 on infarction volume and recovery of function in a focal embolic stroke model. Stroke. 2002 Dec;33(12):3033-7.

RIDADR	NONH for all modes of transport