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 (IC50
s > 10 μ
M) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50
s > 30 μ
M). 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.
All Tocris products are intended for laboratory research use only.
Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists.
Peukert et al.
ACS Med.Chem.Lett., 2014;5:1114
The citations listed below are publications that use Tocris products. Selected citations for TC-G 1008 include:
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