Name | Darapladib |
Synonyms | SB480848 SB 480848 SB 435445 SB-480848 DARAPLADIB Darapladib Darapladib API Darapladib(SB-480848) N-[2-(Diethylamino)ethyl]-N-[4'-(trifluoromethyl)-1,1'-biphenyl-4-ylmethyl]-2-[2-(4-fluorobenzylthio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl]acetamide 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 N-(2-(Diethylamino)ethyl)-2-(2-((4-fluorobenzyl)thio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)-N-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)acetamide |
CAS | 356057-34-6 |
Molecular Formula | C36H38F4N4O2S |
Molar Mass | 666.77 |
Density | 1.25 |
Boling Point | 741.0±70.0 °C(Predicted) |
Solubility | DMSO |
pKa | 9.03±0.10(Predicted) |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
In vitro study | During copper-catalyzed human LDL oxidation, Darapladib prevents lyso-PtdCho generation and subsequent monocyte chemotaxis with an IC50 of 4 nM. |
In vivo study | In WHHL rabbits, Darapladib (30 mg/kg, oral) showed Lp-PLA2 good inhibition of 95% atherosclerosis. Darapladib, as a Lp-PLA inhibitor, attenuates advanced coronary atherosclerosis in pigs with diabetes and hypercholesterolemia (DMHC). In DMHC pigs, darapladib reduced the amount of IgG immunopositive substances permeating the brain and decreased the density of aβ42-containing neurons. |