Bioactivity | 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]. | ||||||||||||
Invitro | 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]. | ||||||||||||
In Vivo | Izencitinib (TD-1473, 1 mg/kg BID) preserves body weight and reduced occult blood scores in a mouse oxazolone colitis model[1]. | ||||||||||||
Name | Izencitinib | ||||||||||||
CAS | 2051918-33-1 | ||||||||||||
Formula | C22H26N8 | ||||||||||||
Molar Mass | 402.50 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |