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(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE

Basic information Safety Supplier Related

(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE Basic information

Product Name:
(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE
Synonyms:
  • (2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE
  • 2-PYRROLIDINECARBOXAMIDE, 1-[(3R)-5-CHLORO-1-[(2,4-DIMETHOXYPHENYL)SULFONYL]-2,3-DIHYDRO-3-(2-METHOXYPHENYL)-2-OXO-1H-INDOL-3-YL]-4-HYDROXY-N,N-DIMETHYL-, (2S,4R)-
  • Nelivaptan
  • Nelivaptan(SSR-149,415)
  • (2S,4R)-1-[(3R)-5-chloro-1-(2,4-dimethoxyphenyl)sulfonyl-3-(2-methoxyphenyl)-2-oxoindol-3-yl]-4-hydroxy-N,N-dimethylpyrrolidine-2-carboxamide
  • SSR 149415
  • (2S,4R)-1-[(3R)-5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-(2-methoxyphenyl)-2-oxo-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide
  • SSR 149415 - Nelivaptan
CAS:
439687-69-1
MF:
C30H32ClN3O8S
MW:
630.11
Mol File:
439687-69-1.mol
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(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE Chemical Properties

Boiling point:
799.7±70.0 °C(Predicted)
Density 
1.414±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
63.01mg/ml in DMSO; 63.01mg/ml in ethanol
pka
14.14±0.40(Predicted)
form 
Solid
color 
White to off-white
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(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDE Usage And Synthesis

Uses

SSR 149415 is a vasopressin V1b receptor antagonist.

Biological Activity

SSR149415 is an orally active, selective vasopressin V1b receptor antagonist (human/r at Ki in nM = 1.5/1.3/V1b, 91/1050/V1a, 1412/2897/V2, 174/270/OT) th at inhibits 30 nM AVP-induced Ca2+ response in human and r at V1b CHO transfectants (Ki = 1.26/2.0 nM). SSR149415 suppresses AVP-mediated physiological responses in vivo, including corticotropin secretion (1-30 mg/kg p.o. or i.p. in rats) upon exogenous AVP administration (0.3 μg/kg alone or 0.03 μg/kg with 0.1 μg corticoliberin/kg via i.v.), restraint stress-Induced corticotropin secretion (EC50 = 10 mg/kg i.p. in rats), and in a murine model of anxiety (four-plate test; 1-10 mg/kg i.p. or 3-10 mg/kg p.o. acute or 10 mg/kg/day p.o.).

storage

Store at -20°C

(2S,4R)-1-[(R)-5-CHLORO-1-(2,4-DIMETHOXY-BENZENESULFONYL)-3-(2-METHOXY-PHENYL)-2-OXO-2,3-DIHYDRO-1H-INDOL-3-YL]-4-HYDROXY-PYRROLIDINE-2-CARBOXYLIC ACID DIMETHYLAMIDESupplier

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