MBX-2982

MBX-2982 is an 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

WARNING This product is not for human or veterinary use.

1. Yang, J.W., Kim, H.S., Im, J.H., et al. GPR119: A promising target for nonalcoholic fatty liver disease. The FASEB Journal 30(1), 324-335 (2016).

2. Lan, H., Lin, H.V., Wang, C.F., et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br. J. Pharmacol. 165(8), 2799-2807 (2012).

3. Spasov, A.A., Kosolapov, V.A., Babkov, D.A., et al. Effect of GRP119 receptor agonist, compound MBX-2982, on activity of human glucokinase. Bull. Exp. Biol. Med. 163(5), 695-698 (2017).