中文名称:

8-氯-4-[(3-氯-4-氟苯基)氨基]-6-[[[1-(1-乙基-4-哌啶)-1H-1,2,3-三唑-4-基]甲基]氨基]-3-喹啉甲腈

中文同义词:

8-氯-4-[(3-氯-4-氟苯基)氨基]-6-[[[1-(1-乙基-4-哌啶)-1H-1,2,3-三唑-4-基]甲基]氨基]-3-喹啉甲腈;8-氯-4-[(3-氯-4-氟苯基)氨基]-6-[[[1-(1-乙基哌啶-4-基)-1H-1,2,3-三唑-4-基]甲基]氨基]喹啉-3-甲腈;COT/TPL2抑制剂(COT INHIBITOR-2)

英文名称:

8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]methyl]amino]-3-Quinolinecarbonitrile

英文同义词:

8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]methyl]amino]-3-Quinolinecarbonitrile;8-Chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]methyl]amino]quinoline-3-carbonitrile;Cot inhibitor-2;3-Quinolinecarbonitrile, 8-chloro-4-[(3-chloro-4-fluorophenyl)aMino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1,2,3-triazol-4-yl]Methyl]aMino]-;8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[[[1-(1-ethyl-4-piperidinyl)-1H-1;COT INHIBITOR2; COT INHIBITOR 2;Tpl2-IN-34

CAS号:

915363-56-3

分子式:

C26H25Cl2FN8

分子量:

539.43

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

915363-56-3.mol

沸点 

713.3±70.0 °C(Predicted)

密度 

1.45

酸度系数(pKa)

8.62±0.10(Predicted)

生物活性

Cot inhibitor-2 是一种有效的，选择性的，具有口服活性的 cot (Tpl2/MAP3K8) 抑制剂，IC50 为 1.6 nM。Cot inhibitor-2 抑制 LPS 刺激的人全血中 TNF-α 的产生，IC50 为 0.3 μM。

靶点

COT/Tpl2

体内研究

Cot inhibitor-2 (compound 34) is orally administered in rats with 100 mg/kg dosing and showed a C max of 517 ng/mL (0.89 μM) and AUC of 4841 ng•h/mL. Cot inhibitor-2 is tested in the LPS-induced TNF-α production model in female Sprague-Dawley rats. With a 25 mg/kg po dose, Cot inhibitor-2 inhibits LPS-induced TNF-α production by 83%.