| Identification | Back Directory | [Name]
BMS 665053 | [CAS]
1173435-64-7 | [Synonyms]
BMS 665053
BMS-665053 >=98% (HPLC)
5-chloro-1-[(1S)-1-cyclopropylethyl]-3-[2,6-dichloro-4-(difluoromethoxy)anilino]pyrazin-2-one
2(1H)-Pyrazinone, 5-chloro-1-[(1S)-1-cyclopropylethyl]-3-[[2,6-dichloro-4-(difluoromethoxy)phenyl]amino]- | [Molecular Formula]
C16H14Cl3F2N3O2 | [MDL Number]
MFCD28977961 | [MOL File]
1173435-64-7.mol | [Molecular Weight]
424.66 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
DMSO: 20mg/mL, clear | [form ]
powder | [color ]
white to light brown | [optical activity]
[α]/D +16 to +21°, c = 0.4 in chloroform-d |
| Hazard Information | Back Directory | [Uses]
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)[1]. | [Biochem/physiol Actions]
BMS-665053 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%). | [References]
[1] Jianqing Li, et al. An Efficient, Direct Bis-ortho-chlorination of 4-(Difluoromethoxy)aniline and Its Application to the Synthesis of BMS-665053, a Potent and Selective Pyrazinone-Containing Corticotropin-Releasing Factor-1 Receptor Antagonist. Organic Process Research & Development, 16, 156-159. |
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