For research use only. Not for therapeutic Use.
Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis[1].
Izencitinib (TD-1473) inhibits cytokine-evoked STAT phosphorylation in human peripheral blood mononuclear cells (PBMCs) and in a human colonic epithelial cell line (pIC50 ≥ 6.7)[1].
Izencitinib (TD-1473) is a potent JAK1, JAK2, JAK3, and TYK2 inhibitor at the human JAK kinase domains (pKi values of 10.0, 10.0, 8.8, and 9.5, respectively)[1].
Izencitinib (TD-1473, 1 mg/kg BID) preserves body weight and reduced occult blood scores in a mouse oxazolone colitis model[1].
| Catalog Number | I029693 |
| CAS Number | 2051918-33-1 |
| Synonyms | 3-[(1R,5S)-3-[[7-[(5-methyl-1H-pyrazol-3-yl)amino]-1,6-naphthyridin-5-yl]amino]-8-azabicyclo[3.2.1]octan-8-yl]propanenitrile |
| Molecular Formula | C22H26N8 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H26N8/c1-14-10-21(29-28-14)26-20-13-19-18(4-2-8-24-19)22(27-20)25-15-11-16-5-6-17(12-15)30(16)9-3-7-23/h2,4,8,10,13,15-17H,3,5-6,9,11-12H2,1H3,(H3,25,26,27,28,29)/t15?,16-,17+ |
| InChIKey | DADAEARVGOQWHV-ALOPSCKCSA-N |
| SMILES | CC1=CC(=NN1)NC2=NC(=C3C=CC=NC3=C2)NC4CC5CCC(C4)N5CCC#N |
| Reference | [1]. Kevin S Currie, et al. Small-molecule agents for the treatment of inflammatory bowel disease. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2034-2041. [2]. William J Sandborn, et al. Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme. J Crohns Colitis. 2020 Sep 16;14(9):1202-1213. [3]. D. Beattie, et al. TD-1473, a novel, potent, and orally administered, GI-targeted, pan-Janus kinase (JAK) inhibitor. Journal of Crohn’s and Colitis, Volume 10, Issue suppl_1, March 2016, Page S123. |
