TC-G 1008

Key Product Details

Product Description

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.

Product Specifications for TC-G 1008

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for TC-G 1008

The following data is based on the product molecular weight 418.90.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

6 5 4 3 2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.39 mL	11.94 mL	23.87 mL
5 mM	0.48 mL	2.39 mL	4.77 mL
10 mM	0.24 mL	1.19 mL	2.39 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 10 publications citing the usage of this product.

• Jing The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs). Eur J Pharmacol 2019 PMID: 31539553
• Peukert Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 2014 PMID: 25313322

Product Documents for TC-G 1008