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AMG 837 calcium hydrate, a potent GPR40 agonist with an EC50 of 13 nM, exhibits high selectivity over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $46 | In Stock | In Stock | |
| 10 mg | $71 | In Stock | In Stock | |
| 25 mg | $152 | In Stock | In Stock | |
| 50 mg | $247 | In Stock | In Stock | |
| 100 mg | $396 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $51 | In Stock | In Stock |
| Description | AMG 837 calcium hydrate, a potent GPR40 agonist with an EC50 of 13 nM, exhibits high selectivity over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM). |
| Targets&IC50 | FFA1/GPR40:13 nM (EC50) |
| In vitro | GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50: 13 nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50s: 23/13 nM). AMG 837 was a partial agonist on GPR40 with maximal activity 85% of that shown by DHA. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50: 3 μM) on the α2-adrenergic receptor [1]. |
| In vivo | In rats, AMG 837 increases insulin release when glucose levels are elevated [2]. |
| Molecular Weight | 950.97 |
| Formula | C52H44CaF6O8 |
| Cas No. | 1259389-38-2 |
| Smiles | [H]O[H].[H]O[H].O=C([O-])C[C@H](C#CC)C1=CC=C(OCC2=CC(C3=CC=C(C(F)(F)F)C=C3)=CC=C2)C=C1.O=C([O-])C[C@H](C#CC)C4=CC=C(OCC5=CC(C6=CC=C(C(F)(F)F)C=C6)=CC=C5)C=C4.[Ca+2] |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (42.06 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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