Chemical Name: N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Biological ActivityTC-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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists.
Peukert et al.
ACS Med.Chem.Lett., 2014;5:1114
The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs).
Jing et al.
Eur J Pharmacol, 2019;
Citations for TC-G 1008
The citations listed below are publications that use Tocris products. Selected citations for TC-G 1008 include:
4 Citations: Showing 1 - 4
Activation of GPR39 with the agonist TC-G 1008 ameliorates ox-LDL-induced attachment of monocytes to endothelial cells.
Authors: Xu Et al.
An agonist of a zinc-sensing receptor GPR39 enhances tight junction assembly in intestinal epithelial cells via an AMPK-dependent mechanism.
Authors: Pongkorpsakol Et al.
Long-lasting antidepressant-like activity of the GPR39 zinc receptor agonist TC-G 1008.
Authors: Starowicz Et al.
Potential antidepressant-like properties of the TC G-1008, a GPR39 (zinc receptor) agonist.
Authors: Mlyniec Et al.
J Affect Disord. 2016;201:179
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