Darapladib

Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities. Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM). It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy. Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.Formal Name: N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-1H-cyclopentapyrimidine-1-acetamide. CAS Number: 356057-34-6. Synonyms: SB-480848. Molecular Formula: C36H38F4N4O2S. Formula Weight: 666.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 245 nm. SMILES: FC1=CC=C(CSC2=NC(C(CCC3)=C3N2CC(N(CC4=CC=C(C5=CC=C(C(F)(F)F)C=C5)C=C4)CCN(CC)CC)=O)=O)C=C1. InChi Code: InChI=1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3. InChi Key: WDPFJWLDPVQCAJ-UHFFFAOYSA-N.