SR 49059

Modify Date: 2025-08-25 04:13:12

SR 49059 Structure
SR 49059 structure
Common Name SR 49059
CAS Number 150375-75-0 Molecular Weight 620.50
Density 1.499g/cm3 Boiling Point 868ºC at 760mmHg
Molecular Formula C28H27Cl2N3O7S Melting Point N/A
MSDS Chinese USA Flash Point 478.8ºC

 Use of SR 49059


SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].

 Names

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
Synonym More Synonyms

 SR 49059 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.499g/cm3
Boiling Point 868ºC at 760mmHg
Molecular Formula C28H27Cl2N3O7S
Molecular Weight 620.50
Flash Point 478.8ºC
Exact Mass 619.09500
PSA 147.85000
LogP 5.08430
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.664
InChIKey CEBYCSRFKCEUSW-NAYZPBBASA-N
SMILES COc1ccc(S(=O)(=O)N2c3ccc(Cl)cc3C(O)(c3ccccc3Cl)C2C(=O)N2CCCC2C(N)=O)cc1OC
Storage condition 2-8°C

 Safety Information

RIDADR NONH for all modes of transport

 Articles28

More Articles
The secretion patterns and roles of cardiac and circulating arginine vasopressin during the development of heart failure.

Neuropeptides 51 , 63-73, (2015)

The aim of this study is to investigate local cardiac and circulating AVP secretion during heart failure and to determine whether AVP mediates ventricular remodeling.We assessed cardiac function and A...

Vasopressin and hydration play a major role in the development of glucose intolerance and hepatic steatosis in obese rats.

Diabetologia 58(5) , 1081-90, (2015)

High plasma copeptin, a marker of vasopressin (VP) secretion, has been shown to be associated with the metabolic syndrome and development of type 2 diabetes in humans. The present study was designed t...

Vasopressin-2 receptor antagonist attenuates the ability of the lungs to clear edema in an experimental model.

Am. J. Respir. Cell. Mol. Biol. 47(5) , 583-8, (2012)

In the last two decades, the role of the alveolar active sodium transport was extensively studied and was found to play a crucial role in regulating alveolar fluid clearance (AFC), and thus in keeping...

 SR 49059Bioassay

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Name: This assay (PMID: 37558952) monitors the impact of a chemical compound on general aut...
Source: ChEMBL
Target: TERT-RPE1
External Id: CHEMBL5724699
Name: This assay (PMID: 37558952) monitors the impact of a chemical compound on general aut...
Source: ChEMBL
Target: U2OS
External Id: CHEMBL5724701
Name: Thermal Shift Assay. Domain: start/stop: M1-L298
Source: ChEMBL
Target: Cyclin-dependent kinase 2
External Id: CHEMBL5062802
Name: This assay (PMID: 37558952) monitors the impact of a chemical compound on ER-phagy fl...
Source: ChEMBL
Target: U2OS
External Id: CHEMBL5724700
Name: Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit...
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
Target: N/A
External Id: HMS1315
Name: Tocris HTS for Inhibitors of Aerobactin Synthetase lucA
Source: 23265
External Id: IucA Pilot Assay Tocris Library
Name: Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste...
Source: Broad Institute
Target: N/A
External Id: 7124-01_Inhibitor_SinglePoint_HTS_Activity
Name: Thermal Shift Assay. Domain: start/stop: M1-S360
Source: ChEMBL
Target: Mitogen-activated protein kinase 1
External Id: CHEMBL5066616
Name: Displacement of [Se-Se]-AVP from human V1A receptor expressed in CHO cells after 4 hr...
Source: ChEMBL
Target: Vasopressin V1a receptor
External Id: CHEMBL4276648
Name: Thermal Shift Assay. Domain: start/stop: M26-R383
Source: ChEMBL
Target: Glycogen synthase kinase-3 beta
External Id: CHEMBL5065589
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 Synonyms

reclovaptan
cis-Ned 19
INDOL-2-YLCARBONYL)-L-PROLINAMIDE
Relcovaptan
SR 49059
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