Tocris Bioscience™ TC-G 1008

Description

Potent and selective GPR39 agonist

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

• Chemical Name or Material: TC-G 1008
• CAS: 1621175-65-2
• Synonym: N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonate
• Quantity: 50 mg
• Solubility: Soluble to 20mM in DMSO
• Molecular Formula: C₁₈H₁₉ClN₆O₂S
• Formula Weight: 418.9
• Physical Form: Solid
• Product Type: Bioactive Small Molecule
• Purity: >98%

Research Use Only. Not For Human or Veterinary Use