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AMG 837 hemicalcium salt
Potent free fatty acid receptor 1 (FFA1/GPR40) partial agonist (EC50 values are 13.5, 22.6 and 31.7 nM at human, mouse and rat receptors, respectively). Interacts allosterically with full FFA1 agonist Docosahexaenoic acid (Cat. No. 3687). Potentiates glucose-dependent stimulation of insulin in vivo. Antidiabetic.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 457.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.19 mL||10.93 mL||21.86 mL|
|5 mM||0.44 mL||2.19 mL||4.37 mL|
|10 mM||0.22 mL||1.09 mL||2.19 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Houze et al (2012) AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg.Med.Chem.Lett. 22 1267 PMID: 22217876
Lin et al (2012) Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol.Pharmacol. 82 843 PMID: 22859723
Lin et al (2011) AMG 837: a novel GPR40/FFA1 agonist that enhances Ins secretion and lowers glucose levels in rodents. PLoS One 6 e27270 PMID: 22087278
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