For research use only. Not for therapeutic Use.
Darapladib (CAT: I003299) is a small molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 is an enzyme involved in the hydrolysis of oxidized phospholipids, leading to the formation of pro-inflammatory and pro-atherogenic molecules. By inhibiting Lp-PLA2, darapladib reduces the production of these harmful molecules and may help in reducing inflammation and preventing the progression of atherosclerosis. Darapladib has been studied for its potential in the treatment of cardiovascular diseases, particularly in patients with coronary artery disease.
| Catalog Number | I003299 |
| CAS Number | 356057-34-6 |
| Synonyms | N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide |
| Molecular Formula | C₃₆H₃₈F₄N₄O₂S |
| Purity | 97% |
| Documentation | |
| Target | Apoptosis |
| Solubility | in DMSO > 10 mM |
| Storage | Store at -20°C |
| Related CAS | 304694-39-1 356058-42-9 2765255-93-2 402-44-8 |
| Overview of Clinical Research | Darapladib is a1-alkyl-2-acetylglycerophosphocholine esterase inhibitor. It has been granted for the new molecular entity. |
| IC50 | 270 pM |
| IUPAC Name | N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide |
| InChI | 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 |
| InChIKey | WDPFJWLDPVQCAJ-UHFFFAOYSA-N |
| SMILES | CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F |
| Reference | 1:Retinal pathology is associated with increased blood-retina barrier permeability in a diabetic and hypercholesterolaemic pig model: Beneficial effects of the LpPLA2 inhibitor Darapladib. Acharya NK, Qi X, Goldwaser EL, Godsey GA, Wu H, Kosciuk MC, Freeman TA, Macphee CH, Wilensky RL, Venkataraman V, Nagele RG.Diab Vasc Dis Res. 2017 May;14(3):200-213. doi: 10.1177/1479164116683149. Epub 2017 Mar 1. PMID: 28301218 |
