Uses
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM[1].
Definition
ChEBI: 8-chloro-4-(3-chloro-4-fluoroanilino)-6-[[1-(1-ethyl-4-piperidinyl)-4-triazolyl]methylamino]-3-quinolinecarbonitrile is an aminoquinoline.
in vivo
Cot inhibitor-2 (compound 34) is orally administered in rats with 100 mg/kg dosing and showed a Cmax 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%[1].
References
[1] Junjun Wu, et al. Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3485-8. DOI:
10.1016/j.bmcl.2009.05.009
![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 Structure](https://www.chemicalbook.com/CAS/GIF/915363-56-3.gif)
