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AMG-837 | Partial agonist of FFAR1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FFAR1
    • EC50:120 nM (Emax 29 %)
    • IC50:7.8 nM
    • EC50:4.8 nM
    Partial agonist
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    Inactive on the closely related GPCRs GPR41 and GPR43. No significant activity in cell-based assa ...

    Potency
    Cellular
    In Vitro

    FFAR1

    Mode of Action: Partial agonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.bmcl.2011.10.118

    In Vivo Validations

    Mouse, Rat, Dog, Cyno
    Dose: 0.8 (M), 0.5 (R) 0.5 (D) 0.5 (C) mg/Kg IV, 5 (M), 0.5 (R) 2 (D) 0.5 (C) mg/Kg PO
    Route of delivery: Intravenous, Oral
    Plasma half life: 8 (M), 7.2 (R), 28 (D), 12.4 (C) h
    Systemic clearance: 0.07 (M), 0.07 (R), 0.08 (D), 0.06 (C) L/h/kg

    DOI Reference: 10.1016/j.bmcl.2011.10.118

    Orthogonal Probes def

    Fasiglifam
    TUG-469

    Chemical Information

    Molecular Formula C26H21F3O3
    SMILEs CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1
    InChI InChI=1S/C26H21F3O3/c1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29/h3,5-15,21H,16-17H2,1H3,(H,30,31)/t21-/m0/s1
    Molecular weight 438.14 Da
    AlogP 0.0
    HBond acceptors 3
    HBond donors 1
    Atoms 53

    References

    Publications

    Cross References

    canSARChEMBLBindingDBPubMed

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 29 Mar 2021 )
    Cellular Use Rating
    In Model Organisms
    FFAR1 (GPR40) is a proposed therapeutic target for the treatment of diabetes due to its ability to mediate glucose stimulated insulin secretion (GSIS) from pancreatic beta-cells and incretin hormones...
    by SERP
    (on 10 Apr 2021 )
    Cellular Use Rating
    In Model Organisms
    My rating refers to using this compound as a partial agonist ONLY. Other compounds are available that display full agonist properties, as described in 10.1371/journal.pone.0046300. Based on the available...
    by SERP
    (on 10 Apr 2021 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria