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    Darapladib (SB-480848)
    Darapladib (SB-480848)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0844
    CAS #: 356057-34-6; Purity ≥98%

    Description: Darapladib (formerly also known as SB-480848; SB 480848; SB480848), a substituted pyrimidone, is a novel, potent and reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with potential anti-inflammatory activity. It inhibits Lp-PLA2 with an IC50 of 0.25 nM. Darapladib is under development in Phase 3 clinical trials for the treatment of atherosclerosis.

    References: Bioorg Med Chem Lett. 2003;13(6):1067-70; Nat Med. 2008;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98.

    Related CAS: 1389264-17-8 (Darapladib-impurity)

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    Molecular Weight (MW)666.77
    FormulaC36H38F4N4O2S
    CAS No.356057-34-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (150.0 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (150.0 mM)
    Other infoChemical 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
    InChi Key: WDPFJWLDPVQCAJ-UHFFFAOYSA-N
    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
    SMILES Code: O=C(N(CCN(CC)CC)CC1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)CN(C3=C4CCC3)C(SCC5=CC=C(F)C=C5)=NC4=O
    SynonymsSB-480848; SB 480848; Darapladib; SB480848


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    In Vitro

    In vitro activity:  During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM.


    Kinase Assay: Darapladib is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with IC50 of 0.25 nM.


    Cell Assay: Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4±3 nM) and subsequent monocyte chemotaxis (IC50=4±1 nM). 

    In VivoIn the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons.
    Animal modelWHHL rabbits 
    Formulation & DosageDissolved in 1% aq methylcellulose; 30 mg/kg; p.o.
    ReferencesBioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70; Nat Med. 2008 Oct;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Darapladib (SB-480848)

    Inhibition of Lp-PLA2 results in fewer lesion macrophages in coronary arteries. Nat Med. 2008 Oct;14(10):1059-66. 
     

    Darapladib (SB-480848)

    Inhibition of Lp-PLA2 results in fewer lesion macrophages in coronary arteries. Nat Med. 2008 Oct;14(10):1059-66.
     

    Darapladib (SB-480848)

    Influence of DM-HC induction and darapladib on arterial phospholipid composition. Nat Med. 2008 Oct;14(10):1059-66.


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