TC-G 1008

Biological Activity

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.

Technical Data

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.

Background References

1. Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists.
   Peukert et al.
   ACS Med.Chem.Lett., 2014;5:1114
2. 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;

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