General description
A cell-permeable pyrimidinylmethyl-pyrimidinone compound that acts as potent, reversible and non-competitive GPR40 antagonist. Selectively blocks GPR40-mediated intracellular Ca2+ release stimulated by GPR40 Agonist GW9508 (Cat. No. 371706) and linoleic acid (pIC50 of 5.99 in GPR40 expressing HEK293 cells) with no effect on GPR120-mediated activation. Shown to significantly reverse glucose-induced insulin secretion potentiated by GW9508 and only partially reduce linoleic acid effect in MIN6 cells.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Stoddart, L.A., et al. 2007. Mol. Pharmacol.71, 994.Briscoe, C.P., et al. 2006. Br. J. Pharmacol.148, 619.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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