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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

    References

    Publications

      Cross References

      canSARChEMBLBindingDB

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      Expert Reviews

      by SERP
      (on 12 Mar 2021 )
      Cellular Use Rating
      In Model Organisms
      ( The reviewer did not leave any 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