AMG 837 hemicalcium salt

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Description: Potent FFA1 (GPR40) partial agonist
Chemical Name: (βS)-β-1-Propyn-1-yl-4-[[4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]methoxy]benzenepropanoic acid hemicalcium salt
Purity: ≥98% (HPLC)
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Citations
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Biological Activity for AMG 837 hemicalcium salt

AMG 837 hemicalcium salt is a 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.

Compound Libraries for AMG 837 hemicalcium salt

AMG 837 hemicalcium salt is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for AMG 837 hemicalcium salt

M. Wt 457.47
Formula C26H20F3O3.½Ca
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1291087-14-3
PubChem ID 46854655
InChI Key WCZAHGONZBHQSA-UHFFFAOYSA-L
Smiles CC#C[C@H](C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)CC([O-])=O.CC#C[C@H](C4=CC=C(C=C4)OCC5=CC=CC(C6=CC=C(C(F)(F)F)C=C6)=C5)CC([O-])=O.[Ca+2]

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.

Solubility Data for AMG 837 hemicalcium salt

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.75 100

Preparing Stock Solutions for AMG 837 hemicalcium salt

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for AMG 837 hemicalcium salt

References for AMG 837 hemicalcium salt

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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Citations for AMG 837 hemicalcium salt

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