Chemical Name: N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Biological ActivityPotent 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. Orally bioavailable.
The technical data provided above is for guidance only.
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
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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