AMG 837 sodium salt
Based on 3 publication(s) in Google Scholar
AMG 837 sodium salt is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 sodium salt stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models. AMG 837 sodium salt binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 sodium salt can be used in research related to type 2 diabetes and brucellosis.
For research use only. We do not sell to patients.
- CAS No.: 865231-45-4
- Formula: C26H20F3NaO3
- Molecular Weight:460.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
AMG 837 sodium salt stimulates inositol phosphate accumulation in A9_GPR40 cells with an EC50 of 7.8 nM[1].
AMG 837 sodium salt potently and selectively stimulates Ca2+ influx mediated by human GPR40 in CHO cells, with an EC50 of 13.5 nM, and shows no activity against the homologous human GPR41, GPR43 or GPR120 receptors[1].
AMG 837 sodium salt activates GPR40 across multiple preclinical species, with EC50 values of 22.6 nM in mice, 31.7 nM in rats, 71.3 nM in dogs, and 30.6 nM in rhesus monkeys in the CHO cell aequorin assay[1].
The potency of AMG 837 sodium salt against human GPR40 decreases in the presence of serum albumin or human serum, with an EC50 value of 210 nM in 0.625% HSA and 2140 nM in 100% human serum[1].
AMG 837 (1 μM) sodium salt enhances insulin secretion activity of primary mouse islets in a glucose-dependent manner[1].
AMG 837 sodium salt inhibits the growth of B. melitensis TZ, B. melitensis M5-90, B. suis S2, and B. abortus A19[2].
AMG 837 (4-16 μg/mL; 6-48 h) sodium salt effectively inhibits B. melitensis TZ in RAW264.7 cells at a concentration of 4 μg/mL, and completely eliminates the bacterium at 16 μg/mL following 6, 12, 24, and 48 h of incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AMG 837 (0.3 mg/kg; p.o.; single administration) sodium salt effectively improves glucose tolerance and increases glucose-stimulated insulin secretion in normal Sprague-Dawley rats even after two consecutive glucose challenges[1].
AMG 837 (0.3-3 mg/kg; p.o.; single administration) sodium salt reduces the postprandial blood glucose AUC0-t by approximately 46% in insulin-resistant Zucker obese rats by enhancing glucose-stimulated insulin secretion[1].
AMG 837 (0.03-0.3 mg/kg; p.o.; once daily for 21 days) sodium salt maintains the efficacy of improving glucose tolerance in insulin-resistant Zucker obese rats, and reduces glucose AUC0-t by 25% at the dose of 0.3 mg/kg on day 21 of administration; its mechanism of action is to continuously stimulate insulin secretion via glucose, without affecting the body weight of rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (8-week-old male)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; single dose
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Result:Did not affect baseline glucose levels 30 minutes post-dose.
Induced a dose-dependent increase in plasma insulin levels, with peak secretion at 5 and 15 minutes post-glucose challenge.
Achieved a half-maximal dose to lower post-prandial glucose of approximately 0.05 mg/kg.
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Animal Model:Sprague-Dawley (8-week-old male)[1]
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Dosage:0.3 mg/kg
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Administration:p.o.; single dose
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Result:Improved blood glucose levels during both glucose challenges, with reduced glucose AUC during each challenge.
Induced peak insulin secretion soon after each glucose administration, mirroring the single-challenge response.
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Animal Model:Zucker fatty (fa/fa) (8-week-old male; insulin-resistant, impaired glucose tolerance model)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Caused baseline glucose levels to trend lower and insulin levels to trend higher 30 minutes post-dose, though neither reached statistical significance.
Reduced post-glucose challenge glucose levels at all doses, with glucose AUC reduced by ~46% for all doses.
Induced a spike in plasma insulin levels 5 and 15 minutes post-glucose challenge at all doses.
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Animal Model:Zucker fatty (fa/fa) (8-week-old male; insulin-resistant, impaired glucose tolerance model)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; daily; 21 days
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Result:On day 1, reduced glucose AUC by 17%, 34% , and 39% at 0.03, 0.1, and 0.3 mg/kg doses, respectively, with corresponding increased insulin secretion post-glucose challenge.
On day 21, reduced glucose AUC by 7%, 15%, and 25% at 0.03, 0.1, and 0.3 mg/kg doses, respectively, with increased insulin secretion in the mid- and high-dose groups post-glucose challenge.
Caused no differences in body weight between treatment and control groups over the 21-day period.
Chemical Information
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CAS No. 865231-45-4
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Molecular Weight 460.42
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Formula C26H20F3NaO3
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SMILES
O=C(O[Na])C[C@H](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2
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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 sodium salt 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].
Lin DC, 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]. Guo KX, et al. High-throughput screening unveils AMG 837 and RORγt 13 as the potent Brucella inhibitor by targeting BacA. Biochem Biophys Res Commun. 2025;757:151624. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AMG 837 sodium salt Related Classifications
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