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.
| 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 | CoA-356057-34-6-M23X12139.pdf |
| 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 2:Predictors of Nonuse of a High-Potency Statin After an Acute Coronary Syndrome: Insights From the Stabilization of Plaques Using Darapladib-Thrombolysis in Myocardial Infarction 52 (SOLID-TIMI 52) Trial. Eisen A, Cannon CP, Braunwald E, Steen DL, Zhou J, Goodrich EL, Im K, Dalby AJ, Spinar J, Daga S, Lukas MA, O/Donoghue ML.J Am Heart Assoc. 2017 Jan 11;6(1). pii: e004332. doi: 10.1161/JAHA.116.004332. PMID: 28077384 Free Article 3:Darapladib, a Lipoprotein-Associated Phospholipase A2 Inhibitor, Reduces Rho Kinase Activity in Atherosclerosis. Zhang J, Xu DL, Liu XB, Bi SJ, Zhao T, Sui SJ, Ji XP, Lu QH.Yonsei Med J. 2016 Mar;57(2):321-7. doi: 10.3349/ymj.2016.57.2.321. PMID: 26847282 Free PMC Article 4:Single and Multiple Dose Pharmacokinetics, Pharmacodynamics and Safety of the Novel Lipoprotein-Associated Phospholipase A2 Enzyme Inhibitor Darapladib in Healthy Chinese Subjects: An Open Label Phase-1 Clinical Trial. Hu C, Tompson D, Magee M, Chen Q, Liu YM, Zhu W, Zhao H, Gross AS, Liu Y.PLoS One. 2015 Oct 14;10(10):e0139862. doi: 10.1371/journal.pone.0139862. eCollection 2015. PMID: 26465780 Free PMC Article 5:The pharmacokinetics and safety of darapladib in subjects with severe renal impairment. Magee MH, Shaddinger B, Collins D, Siddiqi S, Soffer J.Br J Clin Pharmacol. 2015 Oct;80(4):654-61. doi: 10.1111/bcp.12661. Epub 2015 Jul 6. PMID: 25953363 Free PMC Article 6:Darapladib, a lipoprotein-associated phospholipase A2 inhibitor, in diabetic macular edema: a 3-month placebo-controlled study. Staurenghi G, Ye L, Magee MH, Danis RP, Wurzelmann J, Adamson P, McLaughlin MM; Darapladib DME Study Group..Ophthalmology. 2015 May;122(5):990-6. doi: 10.1016/j.ophtha.2014.12.014. Epub 2015 Mar 5. PMID: 25749297 7:Darapladib for the treatment of cardiovascular disease. Campos CM, Suwannasom P, Koenig W, Serruys PW, Garcia-Garcia HM.Expert Rev Cardiovasc Ther. 2015 Jan;13(1):33-48. doi: 10.1586/14779072.2015.986466. Review. PMID: 25521799 8:Acute coronary syndromes: Risk of major coronary events not reduced by darapladib therapy. Duarte JH.Nat Rev Cardiol. 2014 Nov;11(11):621. doi: 10.1038/nrcardio.2014.148. Epub 2014 Sep 16. No abstract available. PMID: 25223450 9:Effect of darapladib on major coronary events after an acute coronary syndrome: the SOLID-TIMI 52 randomized clinical trial. O/Donoghue ML, Braunwald E, White HD, Lukas MA, Tarka E, Steg PG, Hochman JS, Bode C, Maggioni AP, Im K, Shannon JB, Davies RY, Murphy SA, Crugnale SE, Wiviott SD, Bonaca MP, Watson DF, Weaver WD, Serruys PW, Cannon CP; SOLID-TIMI 52 Investigators., Steen DL.JAMA. 2014 Sep 10;312(10):1006-15. doi: 10.1001/jama.2014.11061. Erratum in: JAMA. 2014 Oct 8;312(14):1473. Dylan P. Steen[corrected to Dylan L. Steen]. PMID: 25173516 10:GSK/s darapladib failures dim hopes for anti-inflammatory heart drugs. Mullard A.Nat Rev Drug Discov. 2014 Jul;13(7):481-2. doi: 10.1038/nrd4381. No abstract available. PMID: 24981346 |
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