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Tocris Bioscience™ TC-G 1008
Potent and selective GPR39 agonist
Supplier: Tocris Bioscience™ 5355/10
Description
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.
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.Specifications
TC-G 1008 | |
N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonate | |
Soluble to 100mM in DMSO | |
418.9 | |
Bioactive Small Molecule |
1621175-65-2 | |
10 mg | |
C18H19ClN6O2S | |
Solid | |
>98% |
Safety and Handling
Recommended Storage : Store at 4°C
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Research Use Only. Not For Human or Veterinary Use