1. GPCR/G Protein
  2. GPR40
  3. AMG 837 hemicalcium

AMG 837 hemicalcium 

Cat. No.: HY-129707
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AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1, 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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AMG 837 hemicalcium Chemical Structure

AMG 837 hemicalcium Chemical Structure

CAS No. : 1291087-14-3

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Description

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1, 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].

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 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (%F = 84) and a total plasma Cmax of 1.4 µM[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].

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.
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.
Molecular Weight

457.48

Formula

C₂₆H₂₁F₃O₃.₁/₂Ca

CAS No.

1291087-14-3

SMILES

CC#C[[email protected]@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]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

AMG 837 hemicalciumGPR40Free fatty acid receptor 1FFAR1FFA1G-protein-coupled receptor 40insulinglucoseInhibitorinhibitorinhibit

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AMG 837 hemicalcium
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