Catalog Number: 5355
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.
Background References
  1. Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists.
    Peukert et al.
    ACS Med.Chem.Lett., 2014;5:1114
Citations:

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

1 Citations: Showing 1 - 1

  1. Potential antidepressant-like properties of the TC G-1008, a GPR39 (zinc receptor) agonist.
    Authors: Mlyniec Et al.
    J Affect Disord. 2016;201:179

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