Tocris Bioscience™ TC-G 1008

Descripción

Potent and selective GPR39 agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels in vitro and in vivo. Reduces TNF-α-induced oxidative stress, mitochondrial dysfunction, cytokine expression and secretion of MMPs in fibroblast-like synoviocytes (FLS). Orally bioavailable.

TC-G 1008 is a potent and selective GPR39 agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels in vitro and in vivo. Reduces TNF-α-induced oxidative stress, mitochondrial dysfunction, cytokine expression and secretion of MMPs in fibroblast-like synoviocytes (FLS). Orally bioavailable.