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Tocris Bioscience™ TC-G 1008

Potent and selective GPR39 agonist

Supplier:  Tocris Bioscience™ 5355/10

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Catalog No. 535510


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Description

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

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%
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Safety and Handling

Safety and Handling

Recommended Storage : Store at 4°C

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