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Biological Activity for TC-G 1008
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 for TC-G 1008
|Storage||Store at +4°C|
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.
Solubility Data for TC-G 1008
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TC-G 1008
The following data is based on the product molecular weight 418.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
References for TC-G 1008
References are publications that support the biological activity of the product.
Peukert et al (2014) Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 5 1114 PMID: 25313322
Jing et al (2019) The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs). Eur J Pharmacol 865 172663 PMID: 31539553
If you know of a relevant reference for TC-G 1008, please let us know.
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Keywords: TC-G 1008, TC-G 1008 supplier, TC-G1008, potent, selective, GPR39, zinc, receptor, agonists, agonism, TNF-alpha, alfa, α, rheumatoid, arthritis, Orphan, 7-TM, Receptors, 5355, Tocris Bioscience
4 Citations for TC-G 1008
Citations are publications that use Tocris products. Selected citations for TC-G 1008 include:
Xu et al (2019) Activation of GPR39 with the agonist TC-G 1008 ameliorates ox-LDL-induced attachment of monocytes to endothelial cells. Eur.J.Pharmacol. 858 172451 PMID: 31202806
Mlyniec et al (2016) Potential antidepressant-like properties of the TC G-1008, a GPR39 (zinc receptor) agonist. J Affect Disord. 201 179 PMID: 27235821
Pongkorpsakol et al (2018) An agonist of a zinc-sensing receptor GPR39 enhances tight junction assembly in intestinal epithelial cells via an AMPK-dependent mechanism. Eur.J.Pharmacol. 842 306 PMID: 30459126
Starowicz et al (2018) Long-lasting antidepressant-like activity of the GPR39 zinc receptor agonist TC-G 1008. J.Affect.Disord. 245 325 PMID: 30419533
Do you know of a great paper that uses TC-G 1008 from Tocris? Please let us know.
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Literature in this Area
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