Vercirnon (sodium)

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]. IC50 & Target: IC50: 10 nM (CCR9)^[3] In Vitro: 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]. In Vivo: 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].