AMG 837 hemicalcium
Based on 3 publication(s) in Google Scholar
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.
- CAS No.: 1291087-14-3
- Formula: C26H21F3O3.1/2Ca
- Molecular Weight:457.48
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Biological Activity
pIC50: 8.13 (FFA1)[3]
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.
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.
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Animal Model:8-week old Zucker Fatty Rats[1]
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Dosage:0.03, 0.1, 0.3 mg/kg
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Administration:Oral gavage once daily for 21 days
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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.
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Animal Model:8-week old Sprague-Dawley rats[1]
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Dosage:0.03, 0.1, 0.3 mg/kg
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Administration:A single p.o. administration
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Result:Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
Chemical Information
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CAS No. 1291087-14-3
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Molecular Weight 457.48
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Formula C26H21F3O3.1/2Ca
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Biochem Biophys Res Commun
High-throughput screening unveils AMG 837 and RORγt 13 as the potent Brucella inhibitor by targeting BacA. [Abstract]2025 Apr 9:757:151624. PMID: 40090117
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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Biomed Pharmacother
2023 May:161:114509. PMID: 37002580
Purity & Documentation
References
[1]. Daniel CHL, et, al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011; 6(11): e27270. [Content Brief]
[2]. Houze JB, et, al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15; 22(2): 1267-70. [Content Brief]
[3]. Daniel CHL, et, al. Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol Pharmacol. 2012 Nov;82(5):843-59. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AMG 837 hemicalcium Related Classifications
HY-129707 Related Classifications
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