GPR39-C3

GPR39-C3

CAT N°: 25445
Price:

49.00 41.65

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.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 ?M), ghrelin and neurotensin-1 receptors (IC50s = >30 ?M), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 ?M) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 ?M). 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.

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