| DarapladibLp-PLA2 inhibitor, selective and orally active |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 99.54%
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Chemical structure
| Description | Darapladib (SB-480848) is a reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2)with IC50 of 0.25 nM. | |||||
| Targets | Lp-PLA2 | |||||
| IC50 | 0.25 nM | |||||
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| Cas No. | 356057-34-6 | SDF | Download SDF |
| Synonyms | SB-480848;SB480848;SB 480848 | ||
| Chemical 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 | ||
| Canonical 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 | ||
| Formula | C36H38F4N4O2S | M.Wt | 666.77 |
| Solubility | ≥32.95 mg/mL in DMSO, ≥891 mg/mL in EtOH, <2.52 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. Lipoprotein-associated phospholipase A2 (Lp-PLA2) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. Darapladib is a selective inhibitor of Lp-PLA2.
In vitro: Darapladib potently inhibited Lp-PLA2 with an IC50 of 270 pM. A lack of selectivity against other secretory PLA2s postulated to play a role in atherogenesis had been demonstrated. The percentage inhibition achieved when 1 μM darapladib was evaluated against human secretory PLA2s IIA, V and X, was 0, 0 and 8.7%, respectively [1].
In vivo: Inhibition of lp-PLA2 by darapladib led to attenuation of inflammation in vivo and decreased plaque formation in ApoE-deficient mice, suggesting an anti-atherogenic role during the progression of atherosclerosis [2].
Clinical trial: Darapladib produced sustained inhibition of plasma Lp-PLA2 activity in patients receiving intensive atorvastatin therapy. IL-6 and hs-CRP changes after 12 weeks of darapladib 160 mg suggested a possible reduction in inflammatory burden [3].
References:[1] Bui QT, Wilensky RL. Darapladib. Expert Opin Investig Drugs. 2010;19(1):161-8. [2] Wang WY, Zhang J, Wu WY, Li J, Ma YL, Chen WH, Yan H, Wang K, Xu WW, Shen JH, Wang YP. Inhibition of lipoprotein-associated phospholipase A2 ameliorates inflammation and decreases atherosclerotic plaque formation in ApoE-deficient mice. PLoS One. 2011;6(8):e23425. [3] Mohler ER 3rd, Ballantyne CM, Davidson MH, Hanefeld M, Ruilope LM, Johnson JL, Zalewski A; Darapladib Investigators. The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. J Am Coll Cardiol. 2008;51(17):1632-41.
