TC-G 1008

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

Tocris Bioscience a Bio-Techne Brand

Catalog # 5355

Citations (4)

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Key Product Details

Description:	Potent and selective GPR39 agonist
Chemical Name:	N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	418.9

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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

M. Wt	418.9
Formula	C₁₈H₁₉ClN₆O₂S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1621175-65-2
PubChem ID	91826086
InChi Key	DRSZMILOMUPIBJ-UHFFFAOYSA-N
Smiles	CNC1=NC(NCC2=C(Cl)C=C(NS(C)(=O)=O)C=C2)=CC(C3=NC=CC=C3)=N1

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	41.89	100

Preparing Stock Solutions for TC-G 1008

The following data is based on the product molecular weight 418.9.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.39 mL	11.94 mL	23.87 mL
5 mM	0.48 mL	2.39 mL	4.77 mL
10 mM	0.24 mL	1.19 mL	2.39 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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References for TC-G 1008

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

Jing 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
Peukert Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 2014 PMID: 25313322

Citations for TC-G 1008 (4)

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Citations are publications that use Bio-Techne products. Selected citations for TC-G 1008 include:

Xu et al. (2019) Activation of GPR39 with the agonist TC-G 1008 ameliorates ox-LDL-induced attachment of monocytes to endothelial cells. Eur.J.Pharmacol.. 858:172451
PMID: 31202806
Pongkorpsakol et al. (2018) An agonist of a zinc-sensing receptor GPR39 enhances tight junction assembly in intestinal epithelial cells via an AMPK-dependent mechanism. Eur.J.Pharmacol.. 842:306
PMID: 30459126
Starowicz et al. (2018) Long-lasting antidepressant-like activity of the GPR39 zinc receptor agonist TC-G 1008. J.Affect.Disord.. 245:325
PMID: 30419533
Mlyniec et al. (2016) Potential antidepressant-like properties of the TC G-1008, a GPR39 (zinc receptor) agonist. J Affect Disord.. 201:179
PMID: 27235821

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