TC-G-1008

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TC-G-1008 是一种 GPR39（锌受体）激动剂（大鼠和人类受体的 EC50 值分别为 0.4 和 0.8 nM）。

TC-G-1008, also known as GPR39-C3, is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).

TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM). In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound.

Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively.

GPR39-C3, GPR39 C3, TC-G-1008, TCG1008, TCG 1008

Others

Other Targets

rat GPR39| human GPR39

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1621175-65-2

418.9

C18H19ClN6O2S

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 238.72 mM

CNc2nc(cc(NCc1ccc(NS(C)(=O)=O)cc1Cl)n2)c3ccccn3

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

(-20℃)

With Ice Pack

≥ 2 years