Name: Darapladib
Price: 354.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    SB-480848;SB480848;SB 480848; 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
    
    CAS Number
    
    356057-34-6
    
    Molecular Formula
    
    C36H38F4N4O2S
    
    Molecular Weight
    
    666.77
    
    Appearance
    
    A solid
    
    Purity
    
    99.54%
    
    Solubility
    
    ≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Darapladib

Darapladib

Background

We Also Recommend

Dasatinib hydrochloride

Daun02

DB07268