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Darapladib
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    Darapladib

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    Darapladib
    Darapladib structure.svg
    Clinical data
    Other names SB-480848
    Routes of
    administration
    By mouth
    ATC code
    • None
    Legal status
    Legal status
    • Investigational
    Identifiers
    • N-(2-Diethylaminoethyl)-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
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEMBL
    PDB ligand
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.130.738
    Chemical and physical data
    Formula C36H38F4N4O2S
    Molar mass 666.78 g·mol−1
    3D model (JSmol)
    • FC(F)(F)c1ccc(cc1)c2ccc(cc2)CN(C(=O)CN\4C(\SCc3ccc(F)cc3)=N/C(=O)/C5=C/4CCC5)CCN(CC)CC
    • 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 ☒N
    • Key:WDPFJWLDPVQCAJ-UHFFFAOYSA-N ☒N
     ☒NcheckY (what is this?)  (verify)

    Darapladib is an inhibitor lipoprotein-associated phospholipase A2 (Lp-PLA2) that is in development as a drug for treatment of atherosclerosis.

    It was discovered by Human Genome Sciences in collaboration with GlaxoSmithKline (GSK).

    In November 2013, GSK announced that the drug had failed to meet Phase III endpoints in a trial of 16,000 patients with acute coronary syndrome (ACS). An additional trial of 13,000 patients (SOLID-TIMI 52) finished in May 2014. The study failed to reduce the risk of coronary heart disease death, myocardial infarction, and urgent coronary revascularization compared with placebo in acute coronary syndrome patients treated with standard medical care.



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