Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectively.

Vercirnon (GSK-1605786) sodium inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC 50 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 IC 50 of 141 nM. Vercirnon sodium is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC 50 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]Dosage: 10, 50 mg/kg Administration: Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age Result: Resulted in complete protection from the severe inflammation associated with TNF- overexpression at 50 mg/kg. A similar protective effect was also noted with a lower dose.

886214-18-2

C22H21ClN2NaO4S

467.92

CCX282-Bsodium;GSK-1605786 sodium;维塞诺钠盐;Traficet-ENsodium;Vercirnon sodium

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years