Art. -Nr.: HY-13967

AMG 837

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

AMG 837 is an orally active, selective GPR40/FFA1 agonist with an EC₅₀ of 1.5 nM against human GPR40. AMG 837 stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models. AMG 837 binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 can be used in research related to type 2 diabetes and brucellosis.

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Reinheit: 98.59%
CAS. Nr.: 865231-46-5
Formel: C₂₆H₂₁F₃O₃
Molecular Weight:438.44

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AMG 837 Chemical Structure

CAS. Nr.: 865231-46-5

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A9	EC₅₀	41 nM Compound: 2, AMG 837	Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay	[PMID: 24900872]
CHO	EC₅₀	0.013 μM Compound: AMG 837	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis	[PMID: 26620255]
CHO	EC₅₀	0.06 μM Compound: 1, AMG 837	Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay	[PMID: 24900707]
CHO	EC₅₀	0.06 μM Compound: 1, AMG-837	Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum	[PMID: 24900539]
CHO	EC₅₀	0.08 μM Compound: AMG 837	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin	[PMID: 26620255]
CHO	EC₅₀	104 nM Compound: 2, AMG 837	Agonist activity at human GPR40 expressed in CHO cells by aequorin assay Agonist activity at human GPR40 expressed in CHO cells by aequorin assay	[PMID: 24900872]
CHO	EC₅₀	8.8 μM Compound: AMG 837	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum	[PMID: 26620255]
HEK293	EC₅₀	2.2 nM Compound: AMG-837	Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	[PMID: 27994752]
MIN6	EC₅₀	4.8 nM Compound: 8, AMG-837	Induction of insulin secretion in mouse MIN6 cells Induction of insulin secretion in mouse MIN6 cells	[PMID: 22217876]

In Vitro

AMG 837 stimulates inositol phosphate accumulation in A9_GPR40 cells with an EC₅₀ of 7.8 nM^[1].
AMG 837 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 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 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) enhances insulin secretion activity of primary mouse islets in a glucose-dependent manner^[1].
AMG 837 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) 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.

In Vivo

AMG 837 (0.03-0.3 mg/kg; p.o.; single administration) improves glucose tolerance in a dose-dependent manner in normal Sprague-Dawley rats^[1].
AMG 837 (0.3 mg/kg; p.o.; single administration) 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) reduces the postprandial blood glucose AUC_0-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) maintains the efficacy of improving glucose tolerance in insulin-resistant Zucker obese rats, and reduces glucose AUC_0-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.

Animal Model:

Sprague-Dawley (8-week-old male)^[1]
Dosage:

0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration:

p.o.; single dose
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.

Animal Model:

Sprague-Dawley (8-week-old male)^[1]
Dosage:

0.3 mg/kg
Administration:

p.o.; single dose
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.

Animal Model:

Zucker fatty (fa/fa) (8-week-old male; insulin-resistant, impaired glucose tolerance model)^[1]
Dosage:

0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:

p.o.; single dose
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.

Animal Model:

Zucker fatty (fa/fa) (8-week-old male; insulin-resistant, impaired glucose tolerance model)^[1]
Dosage:

0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration:

p.o.; daily; 21 days
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

CAS. Nr. 865231-46-5
Appearance Oil
Molecular Weight 438.44
Formel C₂₆H₂₁F₃O₃
Color White to off-white
SMILES

OC(C[C@H](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

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 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.
Biomed Pharmacother

The effects of GPR40 agonists on hair growth are mediated by ANGPTL4. [Abstract]

2023 May:161:114509. PMID: 37002580

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (228.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2808 mL

11.4041 mL

22.8081 mL

5 mM

0.4562 mL

2.2808 mL

4.5616 mL

10 mM

0.2281 mL

1.1404 mL

2.2808 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.70 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2808 mL	11.4041 mL	22.8081 mL	57.0203 mL
	5 mM	0.4562 mL	2.2808 mL	4.5616 mL	11.4041 mL
	10 mM	0.2281 mL	1.1404 mL	2.2808 mL	5.7020 mL
	15 mM	0.1521 mL	0.7603 mL	1.5205 mL	3.8014 mL
	20 mM	0.1140 mL	0.5702 mL	1.1404 mL	2.8510 mL
	25 mM	0.0912 mL	0.4562 mL	0.9123 mL	2.2808 mL
	30 mM	0.0760 mL	0.3801 mL	0.7603 mL	1.9007 mL
	40 mM	0.0570 mL	0.2851 mL	0.5702 mL	1.4255 mL
	50 mM	0.0456 mL	0.2281 mL	0.4562 mL	1.1404 mL
	60 mM	0.0380 mL	0.1901 mL	0.3801 mL	0.9503 mL
	80 mM	0.0285 mL	0.1426 mL	0.2851 mL	0.7128 mL
	100 mM	0.0228 mL	0.1140 mL	0.2281 mL	0.5702 mL

Keywords

AMG 837

3 Cited Publications

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AMG 837

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Anti-diabetic Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG 837

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 837

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Anti-diabetic Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG 837

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 837 Related Classifications

HY-13967 Related Classifications