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 (Request formulation change)
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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    5 mg

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    10 mg

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    25 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

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