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Experimental drugs
GW0742
Другие языки:

    GW0742

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    GW0742
    GW0742 skeletal.svg
    Clinical data
    ATC code
    • None
    Legal status
    Legal status
    • Investigational
    Identifiers
    • [4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methyl phenoxy]-acetic acid
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C21H17F4NO3S2
    Molar mass 471.48 g·mol−1
    3D model (JSmol)
    • FC(F)(F)c3c(F)cc(c1nc(c(s1)CSc2cc(c(OCC(=O)O)cc2)C)C)cc3
    • InChI=InChI=1S/C21H17F4NO3S2/c1-11-7-14(4-6-17(11)29-9-19(27)28)30-10-18-12(2)26-20(31-18)13-3-5-15(16(22)8-13)21(23,24)25/h3-8H,9-10H2,1-2H3,(H,27,28)
    • Key:HWVNEWGKWRGSRK-UHFFFAOYSA-N

    GW0742 (also known as GW610742) is a PPARδ/β agonist that is investigated for drug use by GlaxoSmithKline.

    Pharmacology

    Pharmacodynamics

    It is mixed PPAR-B agonist antagonist depending on its dosage. It has weak activity on multiple nuclear receptors as well. It is antagonistic at androgen receptors and VDR. In silico modelling suggest that it has effects on thyroid hormone receptors.

    Chemistry

    Derivatives

    Multiple derivatives of GW0742 core structure has been developed. One of the compound, which has thiazole ring replaced with an oxazole ring inhibited VDR-meditated transcription with IC50 of 660 nM. Other novel analogues which are more potent than GWO742 with reduced toxicity has been developed as well.

    Research

    GW0742 has been shown to ameliorate experimentally induced pancreatitis in mice. It also prevents hypertension in diet induced obese mice. and is investigated as potential antidiabetic drug as well. It is anti-inflammatory agent as well.

    See also



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