TC-G 1008

Name: TC-G 1008
Brand: Tocris Bioscience
SKU: 5355

Tocris Bioscience, part of Bio-Techne | Catalog # 5355

Citations (9)

COA / SDS

Potent and selective GPR39 agonist

Key Product Details

Chemical Name:	N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Purity:	≥98%

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Technical Data
Citations

Biological Activity for TC-G 1008

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.

Technical Data for TC-G 1008

Formula	C₁₈H₁₉ClN₆O₂S
Storage	Store at +4°C
Purity	≥98%
CAS Number	1621175-65-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for TC-G 1008

Solubility

Soluble Soluble to 100 mM in DMSO

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References for TC-G 1008

References are publications that support the biological activity of the product.

Peukert et al. Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett., 2014;5:1114 PMID: 25313322
Jing et al. The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs). Eur J Pharmacol, 2019; PMID: 31539553

TC-G 1008

Tocris Bioscience, part of Bio-Techne | Catalog # 5355

Key Product Details

Biological Activity for TC-G 1008

Technical Data for TC-G 1008

Solubility for TC-G 1008

Dilution Calculator

Reconstitution Calculator

References for TC-G 1008

Product Documents for TC-G 1008

COA

Certificate of Analysis

SDS

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