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AM-1638 | AM-1638 : Full Agonist of FFAR1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 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, Emax:160 nM; 710 nM in 100% human serum; 100 %
    Full Agonist
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    AM-1638 did not activate the receptors GPR41 (FFAR3) and GPR43 (FFAR2) up to 10 µM, but had weak ...

    Potency
    Cellular
    In Vitro

    FFAR1

    Mode of Action: Full Agonist

    Structure-Activity-Relationship data available? No

    In Vivo Validations

    Mouse, Rat, Cyno
    Dose: 1 mg/kg, iv; 5 mg/kg, po (M), 0.5 mg/kg, iv; 2 mg/kg, po (R), 0.5 mg/kg, iv; 2 mg/kg, po (C), up to 100 mg/Kg po
    Route of delivery: Intravenous, Oral
    Plasma half life: 2.0 (M), 1.8 (R), 2.1 (C) h
    Systemic clearance: 0.18 (M), 0.91 (R), 0.81 (C) L/h/Kg

    Reference: --

    Orthogonal Probes def

    Fasiglifam
    TUG-469
    AMG-837

    Chemical Information

    Molecular Formula C33H35FO4
    SMILEs COc1ccc(F)c(-c2ccc(COc3cccc([C@@H](CC(=O)O)C4CC4)c3)cc2C2=CCCC2(C)C)c1
    InChI InChI=1S/C33H35FO4/c1-33(2)15-5-8-30(33)28-16-21(9-13-26(28)29-18-24(37-3)12-14-31(29)34)20-38-25-7-4-6-23(17-25)27(19-32(35)36)22-10-11-22/h4,6-9,12-14,16-18,22,27H,5,10-11,15,19-20H2,1-3H3,(H,35,36)/t27-/m0/s1
    Molecular weight 514.25 Da
    AlogP 8.252
    HBond acceptors 4
    HBond donors 1
    Atoms 73

    Vendors

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    Expert Reviews

    by SERP
    (on 12 Mar 2021)
    Cellular Use Rating
    In Model Organisms
    (The reviewer did not leave any public comments)
    by SERP
    (on 10 Apr 2021)
    Cellular Use Rating
    There is not enough information on this compound. I would like to see full dose-response curves along with untransfected controls and orthogonal assay system.
    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