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

M.Wt:
418.9
Formula:
C18H19ClN6O2S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1621175-65-2

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 / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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

If you know of a relevant reference for TC-G 1008 please let us know.

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

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