TC-G 1008

Cat. No. 5355 4 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective GPR39 agonist

化学名： N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide

纯度： ≥98% (HPLC)

引用文献 (4)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

化合物库 for TC-G 1008

TC-G 1008 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for TC-G 1008

分子量	418.9
公式	C₁₈H₁₉ClN₆O₂S
储存	Store at +4°C
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for TC-G 1008

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	41.89	100

制备储备液 for TC-G 1008

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for TC-G 1008

分析证书/产品说明书

化学品安全技术说明书

参考文献 for TC-G 1008

参考文献是支持产品生物活性的出版物。

Peukert et al (2014) Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 5 1114 PMID: 25313322

Jing et al (2019) The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs). Eur J Pharmacol 865 172663 PMID: 31539553

If you know of a relevant reference for TC-G 1008, please let us know.

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