Vercirnon(GSK-1605786)sodium是一种具有口服活性的，选择性的CCR9拮抗剂。Vercirnonsodium抑制CCR9介导的Molt-4细胞上Ca2+移动和趋化性，IC50值分别为5.4和3.4nM。Vercirnonsodium对CCR9的选择性高于CCR1-12和CX3CR1-7(IC50s=>10µM)。Vercirnonsodium是CCR9的两种剪接形式(CCR9A和CCR9B)的CCL25定向趋化性的等效抑制剂，IC50值分别为2.8和2.6nM。
货号:ajcx31648
CAS:886214-18-2
分子式:C22H20ClN2NaO4S
分子量：466.91
溶解度:DMSO: 100 mg/mL (214.17 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively[1].

Vercirnon (GSK-1605786) sodium inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. Vercirnon sodium inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon sodium inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC50 of 141 nM. Vercirnon sodium is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC50 values of 6.9 nM and 1.3 nM, respectively[1].

Vercirnon (GSK1605786A) sodium (10, 50 mg/kg; s.c.; twice per day; starting at 2 weeks of age until 12 weeks of age) ameliorates the severity of intestinal inflammation in the TNFδARE mouse model[1]. Animal Model: C57BL/6 mice (TNFδARE Mouse Model of Terminal Ileitis)[1]

[1]. Walters MJ, et al. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther. 2010 Oct;335(1):61-9. [2]. Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340. [3]. Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4.