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AM-5262 | Agonist of FFAR1
RATINGS:
Cellular Use: (1 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
    • EC50:81 nM
    Agonist
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Panel screen data against 101 receptors: CEREP
    Selectivity Assessment Description:
    % of inhibition higher than 70% for 5/101: A3R_Human 97%; TXA2 synthetase_Human 88%; COX2_ACE 85%; C ...

    Potency
    Cellular
    In Vitro

    FFAR1

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300427u

    In Vivo Validations

    Rat
    Dose: 0.5 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 4.2 h
    Systemic clearance: 0.25 L/h/kg
    Volume of Distribution at Steady-State: 0.7 L/kg

    DOI Reference: 10.1021/ml300427u

    Dose: 2 mg/Kg
    Route of delivery: Oral
    Bioavailability: 28%

    DOI Reference: 10.1021/ml300427u

    Monkey (Cynomolgus)
    Dose: 0.5 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 2.2 h
    Systemic clearance: 0.84 L/h/kg
    Volume of Distribution at Steady-State: 1.4 L/Kg

    DOI Reference: 10.1021/ml300427u

    Dose: 2 mg/Kg
    Route of delivery: Oral
    Bioavailability: 69 %

    DOI Reference: 10.1021/ml300427u

    Chemical Information

    Molecular Formula C33H35FO4
    SMILEs COc1ccc(F)c(-c2ccc(COc3ccc4c(c3)[C@]3(CC4)C[C@H]3C(=O)O)cc2[C@@H]2CCCC2(C)C)c1
    InChI InChI=1S/C33H35FO4/c1-32(2)13-4-5-27(32)25-15-20(6-10-24(25)26-16-22(37-3)9-11-30(26)34)19-38-23-8-7-21-12-14-33(28(21)17-23)18-29(33)31(35)36/h6-11,15-17,27,29H,4-5,12-14,18-19H2,1-3H3,(H,35,36)/t27-,29-,33-/m0/s1
    Molecular weight 514.25 Da
    AlogP 7.6625
    HBond acceptors 4
    HBond donors 1
    Atoms 73

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews

    by SERP
    (on 30 Nov 2021)
    Cellular Use Rating
    In Model Organisms
    (The reviewer did not leave any public comments)
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