A reversible inhibitor of Lp-PLA2
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Darapladib

Item No. 16429

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
356057-34-6
Synonyms
  • SB-480848
Molecular Formula
C36H38F4N4O2S
Formula Weight
666.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
245 nm
SMILES
FC1=CC=C(CSC2=NC(C(CCC3)=C3N2CC(N(CC4=CC=C(C5=CC=C(C(F)(F)F)C=C5)C=C4)CCN(CC)CC)=O)=O)C=C1
InChi Code
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
InChi Key
WDPFJWLDPVQCAJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.1,2 Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).3 It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.4 Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Marathe, G.K., Pandit, C., Lakshmikanth, C.L., et al. To hydrolyse or not to hydrolyse: The dilemma of platelet activating factor acetylhydrolase (PAF-AH). J. Lipid Res. 55(9), 1847-1854 (2014).

    2. Stafforini, D.M., and Zimmerman, G. Unraveling the PAF-AH/Lp-PLA2 controversy. J. Lipid Res. 55(9), 1811-1814 (2014).

    3. Blackie, J.A., Bloomer, J.C., Brown, M.J., et al. The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg. Med. Chem. Lett. 13(6), 1067-1070 (2003).

    4. Mohler, E.R., III, Ballantyne, C.M., Davidson, M.H., et al. 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. 51(17), 1632-1641 (2008).

    5. Serruys, P.W., García-García, H.M., Buszman, P., et al. Effects of the direct lipoprotein-associated phospholipase A2 inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 118(11), 1172-1182 (2008).

    6. Wilensky, R.L., Shi, Y., Mohler, E.R., III, et al. Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development. Nat. Med. 14(10), 1059-1066 (2008).