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

AMG 837 hemicalcium 

Cat. No.: HY-129707
Handling Instructions

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.

For research use only. We do not sell to patients.

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. 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]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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AMG 837 hemicalcium Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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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