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首页-小分子抑制剂&激动剂-GPCR-GPR39-TC-G 1008
TC-G 1008

Chemical Structure : TC-G 1008

CAS No.: 1621175-65-2

TC-G 1008 (TC-G-1008, GPR39-C3)

货号: PC-60593Not For Human Use, Lab Use Only.

TC-G 1008 (TC-G-1008, GPR39-C3) is a potent, selective, orally bioavailable GPR39 agonist with EC50 of 0.4 and 0.8 nM for rat and human GPR39, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TC-G 1008 (TC-G-1008, GPR39-C3) is a potent, selective, orally bioavailable GPR39 agonist with EC50 of 0.4 and 0.8 nM for rat and human GPR39, respectively.
TC-G 1008 displays high selectivity over a broad panel of kinases (IC50> 10 uM), and ghrelin and neurotensin-1 receptors (IC50>30 uM).
TC-G 1008 robustly induces acute GLP-1 levels and shows the potential oral treatment of type 2 diabetes.

物理化学性质&存储条件

分子量 418.9
分子式 C18H19ClN6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Młyniec K, et al. J Affect Disord. 2016 Sep 1;201:179-84.

2. Sato S, et al. Mol Pharmacol. 2016 Dec;90(6):726-737.

3. Shimizu Y, et al. Biochem Pharmacol. 2017 Sep 15;140:105-114.

4. Peukert S, et al. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8.

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