Name: BMS-665053
Rating: 5 (10 reviews)

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HIT ID:HIT212712282
Cas No:1173435-64-7
常用名:BMS-665053
别名:BMS665053
IUPAC:5-chloro-1-[(1S)-1-cyclopropylethyl]-3-{[2,6-dichloro-4-(difluoromethoxy)phenyl]amino}-1,2-dihydropyrazin-2-one
IUPAC:5-chloro-1-[(1S)-1-cyclopropylethyl]-3-{[2,6-dichloro-4-(difluoromethoxy)phenyl]amino}-1,2-dihydropyrazin-2-one
InChI key:NFRNVFLIULAQST-ZETCQYMHSA-N

分子式:C16H14Cl3F2N3O2
分子量:424.65
氢键供体数 (HBD):1
氢键受体数 (HBA):4
LogP:5.0776772
SMILES:C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O
SMILES:C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O

BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addition, BMS-665053 is efficacious in the Defensive Withdrawal model of anxiety in rats and has low in vivo clearance (Cl = 17 mL/min/kg, t½ = 7.8 h) in rats.

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