AMG 837 calcium hydrate
Based on 3 publication(s) in Google Scholar
AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models. AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 1259389-38-2
- Formula: C26H21F3O3.1/2Ca.H2O
- Molecular Weight:455.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) AMG 837 calcium hydrate
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Customer Validation & Images
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Cell Imaging/Staining
Biological Activity
pIC50: 8.13 (FFA1)[3]
AMG 837 calcium hydrate stimulates inositol phosphate accumulation in A9_GPR40 cells with an EC50 of 7.8 nM[1].
AMG 837 calcium hydrate 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 calcium hydrate 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 calcium hydrate 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) calcium hydrate enhances insulin secretion activity of primary mouse islets in a glucose-dependent manner[1].
AMG 837 calcium hydrate 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) calcium hydrate 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) calcium hydrate 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) calcium hydrate 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) calcium hydrate 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, 0.1, 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:0.03, 0.1, 0.3 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:0.03, 0.1, 0.3 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. 1259389-38-2
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Appearance Solid
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Molecular Weight 455.45
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Formula C26H21F3O3.1/2Ca.H2O
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Color White to off-white
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SMILES
OC(C[C@H](C#CC)C(C=C1)=CC=C1OCC2=CC=CC(C3=CC=C(C=C3)C(F)(F)F)=C2)=O.[Ca].O.[1/2]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 -
Biomed Pharmacother
2023 May:161:114509. PMID: 37002580 -
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 calcium hydrate 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.
Solvent & Solubility
DMSO : ≥ 42 mg/mL (92.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. 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 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.49 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 | 2.1956 mL | 10.9782 mL | 21.9563 mL | 54.8908 mL |
| 5 mM | 0.4391 mL | 2.1956 mL | 4.3913 mL | 10.9782 mL | |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1956 mL | 5.4891 mL | |
| 15 mM | 0.1464 mL | 0.7319 mL | 1.4638 mL | 3.6594 mL | |
| 20 mM | 0.1098 mL | 0.5489 mL | 1.0978 mL | 2.7445 mL | |
| 25 mM | 0.0878 mL | 0.4391 mL | 0.8783 mL | 2.1956 mL | |
| 30 mM | 0.0732 mL | 0.3659 mL | 0.7319 mL | 1.8297 mL | |
| 40 mM | 0.0549 mL | 0.2745 mL | 0.5489 mL | 1.3723 mL | |
| 50 mM | 0.0439 mL | 0.2196 mL | 0.4391 mL | 1.0978 mL | |
| 60 mM | 0.0366 mL | 0.1830 mL | 0.3659 mL | 0.9148 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6861 mL |
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