1621175-65-2

GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC₅₀ values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively. It is selective for GPR39 over a panel of kinases (IC₅₀s = >10 μM), ghrelin and neurotensin-1 receptors (IC₅₀s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; ) in STC-1 mouse enteroendocrine cells (EC₅₀ = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC₅₀ = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.

TC-G 1008 is the first potent, selective, and orally bioavailable GPR39 agonist.

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