CAS 150375-75-0|SR 49059
| 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 | / |
| MSDS | ChineseUSA | Flash Point | 478.8ºC |
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 BiologicalActivity
| Description | SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1]. |
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| Related Catalog | Research Areas >>Cardiovascular DiseaseResearch Areas >>EndocrinologySignaling 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. |
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 |
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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... |
Synonyms
| reclovaptan |
| cis-Ned 19 |
| INDOL-2-YLCARBONYL)-L-PROLINAMIDE |
| Relcovaptan |
| SR 49059 |
