Description
BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist. BMS-665053)11 had high affinity for the CRF1 receptor (IC50 = 1.0 nM) and was a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM), indicating that it behaved as an antagonist. In addition, BMS-665053 was efficacious in the Defensive Withdrawal model of anxiety in rats and had low in vivo clearance (Cl = 17 mL/min/kg, t½ = 7.8 h) in rats.
Chemical Formula
C16H14Cl3F2N3O2
Molecular Weight
424.6538
Elemental Analysis
C, 45.25; H, 3.32; Cl, 25.04; F, 8.95; N, 9.90; O, 7.54
Synonym
BMS-665053; BMS 665053; BMS665053.
IUPAC/Chemical Name
(S)-5-chloro-1-(1-cyclopropylethyl)-3-((2,6-dichloro-4-(difluoromethoxy)phenyl)amino)pyrazin-2(1H)-one
InChi Key
NFRNVFLIULAQST-ZETCQYMHSA-N
InChi Code
InChI=1S/C16H14Cl3F2N3O2/c1-7(8-2-3-8)24-6-12(19)22-14(15(24)25)23-13-10(17)4-9(5-11(13)18)26-16(20)21/h4-8,16H,2-3H2,1H3,(H,22,23)/t7-/m0/s1
SMILES Code
ClC1=CC(OC(F)F)=CC(Cl)=C1NC2=NC(Cl)=CN([C@@H](C)C3CC3)C2=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).
HS Tariff Code
2934.99.9001