(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
(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 Basic information
- Product 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
- Synonyms:
-
- (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
- INDOL-2-YLCARBONYL)-L-PROLINAMIDE
- Relcovaptan
- reclovaptan
- SR 49059
- Relcovaptan (SR-49059)
- 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)-
- CAS:
- 150375-75-0
- MF:
- C28H27Cl2N3O7S
- MW:
- 620.5
- Mol File:
- 150375-75-0.mol
(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 Chemical Properties
- 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
(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 Usage And Synthesis
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
(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-PYRROLIDINECARBOXAMIDESupplier
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 1-631-485-4226; 16314854226
- info@bocsci.com
- Tel
- 010-56205725
- waley188@sohu.com
- Tel
- 021-61415566 800-8193336
- orderCN@merckgroup.com
- Tel
- 888-539-0666
- info@emmx.com
(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(150375-75-0)Related Product Information
- 2-amino-5-chloro-diphenyl methanol
- 1R,2S-(-)-Norephedrine hydrochloride
- (1S,2S)-(+)-Pseudoephedrine hydrochloride
- Norpseudoephedrine hydrochloride
- (S)-(-)-2-AMINO-1,1-DIPHENYL-1-PROPANOL
- (R)-1-(3-CHLOROPHENYL)-1-HYDROXY-2-AMINOETHANE
- 2-CHLORO-ALPHA-[2-DIMETHYLAMINOETHYL]BENZHYDROL HYDROCHLORIDE
- H-D-VAL-NH2 HCL
- CHEMBRDG-BB 7436664
- (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-chloroamphetamine
- 2-[(3,3-DIPHENYLPROPYL)AMINO]ACETAMIDE HYDROCHLORIDE
- (1S,2S)-(+)-PSEUDOEPHEDRINE-D3 HCL (N-METHYL-D3)
- (S)-(-)-1,1-DIPHENYL-2-AMINOPROPANE
- (+)-a-Aminomethyl-o-chlorobenzyl alcohol
- 2-AMINO-1-(3-CHLORO-PHENYL)-ETHANOL HCL
- (R)-2-AMINO-1-(3-CHLOROPHENYL) ETHANOL HYDROCHLORIDE
- Benzenemethanol, a-(aminomethyl)-2-chloro-, hydrochloride, (S)-