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MEDICA 16 is a G protein-coupled receptor 40 (GPR40) agonist and GPR120 partial agonist.1 MEDICA 16 induces intracellular calcium mobilization in cells expressing GPR40 or GPR120 in a concentration-dependent manner. It induces ERK activation in cells expressing GPR40 or GPR120 when used at a concentration of 100 µM. MEDICA 16 also inhibits ATP citrate lyase (Kis = 40 and 200 µM for the oxidized and reduced enzyme, respectively).2 Chronic dietary administration of MEDICA 16 (0.25% w/w) decreases liver acetyl-CoA carboxylase (ACC) and AMP-activated protein kinase (AMPK) levels in a model of insulin resistance using JCR:LA-cp rats, which lack functioning leptin receptors.3 MEDICA 16 (0.25% w/w in the diet) reduces plasma insulin levels, decreases fasting plasma triacylglycerol levels, and delays the onset of hyperinsulinemia in JCR:LA-cp rats.4
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1. Novel selective ligands for free fatty acid receptors GPR120 and GPR40. Naunyn Schmiedebergs Arch Pharmacol. 380(3), 247-255 (2009).
2. Redox control of catalysis in ATP-
3. MEDICA 16 inhibits hepatic acetyl-
4. Development of insulin resistance in the JCR:LA-