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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 | Availability | Quantity |
---|---|---|---|
2 mg | $31 | In Stock | |
5 mg | $48 | In Stock | |
10 mg | $73 | In Stock | |
25 mg | $153 | In Stock | |
50 mg | $298 | In Stock | |
100 mg | $437 | In Stock | |
200 mg | $597 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | 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. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (87.83 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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