1. GPCR/G Protein
  2. Free Fatty Acid Receptor
  3. AMG 837 hemicalcium

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.

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CAS No. : 1291087-14-3

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    AMG 837 hemicalcium purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2025 Apr 9:757:151624.  [Abstract]

    Ability of different concentrations compounds or drugs (GM, Gentamicin, Sterile; AMG 837; RORγt 13; RIF; 4, 16 μg/mL) to clear B. melitensis TZ in RAW264.7 cells at 24 h. Cells appear blue; B. melitensis TZ appear green.

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    Description

    AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents[1][2][3].

    IC50 & Target

    pIC50: 8.13 (FFA1)[3]

    In Vitro

    AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice[1].
    AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats[1].
    AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo[1].
    AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma Cmax of 1.4 µM[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 8-week old Zucker Fatty Rats[1]
    Dosage: 0.03, 0.1, 0.3 mg/kg
    Administration: Oral gavage once daily for 21 days
    Result: Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.
    Increased insulin levels in the mid- and high-dose groups.
    Not affected body weights during the 21-day treatment.
    Animal Model: 8-week old Sprague-Dawley rats[1]
    Dosage: 0.03, 0.1, 0.3 mg/kg
    Administration: A single p.o. administration
    Result: Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
    Molecular Weight

    457.48

    Formula

    C26H21F3O3.1/2Ca

    CAS No.
    SMILES

    CC#C[C@@H](CC([O-])=O)C1=CC=C(OCC2=CC=CC(C3=CC=C(C=C3)C(F)(F)F)=C2)C=C1.[Ca+2].[1/2]

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    Room temperature in continental US; may vary elsewhere.

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    Please store the product under the recommended conditions in the Certificate of Analysis.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    AMG 837 hemicalcium
    Cat. No.:
    HY-129707
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