Pricing updated 2019-07-17. Prices are subject to change without notice.
MBX-2982 is a agonist of GPR119.1 It reduces nuclear and total protein levels of sterol regulatory element binding protein 1 (SREBP-1) in HepG2 cells and rat primary hepatocytes under high-glucose and -insulin conditions and increases phosphorylation of the inhibitory form, SREBP-1c. MBX-2982 (10 mg/kg) inhibits hepatic lipid accumulation in wild-type, but not GPR119 knockout, mice fed a high-fat diet. It also increases plasma levels of glucagon-like peptide 1 (GLP-1; Item No. 24460) in mice when administered at a dose of 10 mg/kg prior to, and to a greater extent following, glucose administration.2 MBX-2982 increases glucokinase activity in an enzyme assay with an EC50 value of 45.11 µM.3
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1. Yang, J.W., Kim, H.S., Im, J.H., et al. GPR119: A promising target for nonalcoholic fatty liver disease FASEB J. 30(1), 324-335 (2016).
Lan, H., Lin, H.V., Wang, C.F., et al. Agonists at GPR119 mediate secretion of GLP-
Spasov, A.A., Kosolapov, V.A., Babkov, D.A., et al. Effect of GRP119 receptor agonist, compound MBX-