TC-G 1008

Cat. No. 5355

TC-G 1008 C18H19ClN6O2S [1621175-65-2]

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Chemical Name: N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide

Biological Activity

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. Orally bioavailable.

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

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Peukert et al (2014) Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 5 1114. PMID: 25313322.

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Citations are publications that use Tocris products. Selected citations for TC-G 1008 include:

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.

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View Related Products by Product Action

Keywords: TC-G 1008, supplier, TC-G1008, potent, selective, GPR39, agonists, agonism, Tocris Bioscience, Orphan 7-TM Receptor Agonist products

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