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TGR5 agonist MN6

Chemical Structure : TGR5 agonist MN6

CAS No.: 1315468-57-5

TGR5 agonist MN6

Catalog No.: PC-20412Not For Human Use, Lab Use Only.

TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.

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    Biological Activity

    TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.
    MN6 shows EC50 values of 1.5 and 18 nM on hTGR5 and mTGR5, respectively, by a CRE-driven luciferase reporter gene assay in either the hTGR5/CRE/HEK293 or mTGR5/CRE/HEK293 stable cell line.
    MN6 significantly promoted GLP-1 secretion in human enteroendocrine NCI-H716 cells in a dose-dependent manner.
    MN6 increased the plasma active GLP-1 level in CD1 mice following a glucose bolus, with a 68.5% or 89.3% increase after a single dose of 50 or 100 mg/kg MN6, respectively.
    MN6 exhibited a synergistic effect combined with DPP-4 inhibitor BI-1356 (Cat. PC-42508).
    MN6 (50 mg/kg) improved glucose homeostasis in ob/ob mice, improved metabolic abnormalities and increased the insulinstimulated glucose uptake in the skeletal muscles of DIO mice.

    Physicochemical Properties

    M.Wt 440.32
    Formula C23H19Cl2N3O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dichlorophenoxy)pyridin-3-yl)methanone

    References

    1. Suling Huang, et al. Metabolism. 2019 Oct;99:45-56.

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