AMG837GPR40 agonist,orally bioavailable CAS# 865231-46-5 |
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Quality Control & MSDS
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| Cas No. | 865231-46-5 | SDF | Download SDF |
| PubChem ID | 46854655 | Appearance | Powder |
| Formula | C26H21F3O3 | M.Wt | 438.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Chemical Name | (3S)-3-[4-[[3-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]hex-4-ynoic acid | ||
| SMILES | CC#CC(CC(=O)O)C1=CC=C(C=C1)OCC2=CC=CC(=C2)C3=CC=C(C=C3)C(F)(F)F | ||
| Standard InChIKey | ZOPNBMMVVZRSGH-NRFANRHFSA-N | ||
| Standard InChI | InChI=1S/C26H21F3O3/c1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29/h3,5-15,21H,16-17H2,1H3,(H,30,31)/t21-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
IC50 value: 13 nM (EC50) [1]
Target: GPR40 agonist
AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showed
no significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potent
and selective in vitro. References: | |||||
AMG837 Dilution Calculator
AMG837 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2808 mL | 11.4041 mL | 22.8081 mL | 45.6163 mL | 57.0203 mL |
| 5 mM | 0.4562 mL | 2.2808 mL | 4.5616 mL | 9.1233 mL | 11.4041 mL |
| 10 mM | 0.2281 mL | 1.1404 mL | 2.2808 mL | 4.5616 mL | 5.702 mL |
| 50 mM | 0.0456 mL | 0.2281 mL | 0.4562 mL | 0.9123 mL | 1.1404 mL |
| 100 mM | 0.0228 mL | 0.114 mL | 0.2281 mL | 0.4562 mL | 0.5702 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AMG 837 is a potent and orally bioavailable GPR40 agonist (EC50=14nM). [1]
GPR40 is a G protein-coupled receptor that is activated by free fatty acid. It is located on the cell surface of pancreatic beta-cells, gastrointestinal enteroendocrine cells and immune cells etc. GPR40 is reported to be related the stimulation effects of fatty acids on insulin and incretin secretion. [2]
AMG 837 treatment on GPR40 containing cell membrane increases [35S]-GTPγ binding (EC=1.5±0.1 nM). AMG 837 also stimulates Ca2+ influx (EC50 = 13.5±0.8 nM) in CHO cells transfected with GPR40 and aequorin. [2]
The insulin secretion is stimulated and the postprandial glucose level is lowered in 8-week old Sprague-Dawley rats orally treated with AMG 837. In Zucker fatty rats treated with AMG 837 daily for 21-days shows decreased glucose excursions and elevated glucose stimulated insulin secretion in glucose tolerance tests. [2]
References:
1. Houze JB, Zhu L, Sun Y et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.
2. Lin DC, Zhang J, Zhuang R 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.
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AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
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