| Identification | Back Directory | [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 | [CAS]
150375-75-0 | [Synonyms]
SR 49059
Relcovaptan
reclovaptan
Relcovaptan (SR-49059)
INDOL-2-YLCARBONYL)-L-PROLINAMIDE
(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
2-Pyrrolidinecarboxamide, 1-[[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-, (2S)- | [Molecular Formula]
C28H27Cl2N3O7S | [MDL Number]
MFCD00922133 | [MOL File]
150375-75-0.mol | [Molecular Weight]
620.5 |
| Chemical Properties | Back Directory | [Melting point ]
158-160oC | [Boiling point ]
868.0±75.0 °C(Predicted) | [density ]
1.499±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [pka]
10.95±0.40(Predicted) | [color ]
white to off-white | [optical activity]
[α]/D -180 to -190°, c = 0.3 in chloroform-d | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Uses]
Relcovaptan is a selective vasopressin-1a receptor antagonist that prevents cellular swelling and provides treatment for post-traumatic brain edema. | [Definition]
ChEBI: (2S)-1-[[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxyphenyl)sulfonyl-3-hydroxy-2H-indol-2-yl]-oxomethyl]-2-pyrrolidinecarboxamide is a proline derivative. | [Biological Activity]
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 (IC 50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo . | [Biochem/physiol Actions]
SR 49059 is a potent and selective Arginine Vasopressin (AVP) V1a-receptor antagonist. AVP is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes V1a, V1b, and V2. All belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF. SR 49059 has also shown initial positive results in the treatment of Raynaud′s disease, dysmenorrhoea, and tocolysis. | [storage]
Store at +4°C |
|
| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Sigma-Aldrich
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021-61415566 800-8193336 |
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https://www.sigmaaldrich.cn |
| Company Name: |
DC Chemicals
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021-58447131 13564518121 |
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https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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