Vercirnon 是可口服的选择性CCR9拮抗剂，可抑制 CCR9 介导的 Molt-4 细胞上 Ca2+移动和趋化性，用于炎症性肠病的研究。

Vercirnon is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

Vercirnon is also a potent inhibitor of CCL25-induced Molt-4 chemotaxis (IC50: 3.5 ± 0.3 nM). Vercirnon inhibits CCL25-induced calcium mobilization (IC50: 5.4 ± 0.7 nM). Vercirnon inhibits the chemotaxis of Baf-3/CCR9A cells as well as Baf-3/CCR9A cells (IC50s: 2.8 ± 1.1 nM and 2.6 ± 0.7 nM, respectively). Vercirnon potently inhibits CCL25-induced chemotaxis (IC50: 6.8 ± 1.7 nM in the buffer) and exhibits inhibition on RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum (IC50: 141 ± 13 nM). Vercirnon shows inhibitory activity against Molt-4 migration (IC50: 33.4 ± 1.3 nM in 100% human AB serum). Vercirnon suppresses the binding of [3H] CCX807 to Molt-4 cells (IC50: 6 nM) [1].

Vercirnon (50?mg/kg c.c. twice daily) blocks the colitis-associated weight loss inherent in the mdr1a?/? model and also abrogates growth arrest in the colitis mdr1a ?/? mice. Vercirnon (10, 50 mg/kg twice daily) protects from the severe inflammation associated with TNF-α overexpression in the TNFΔARE Mouse Model [2].

698394-73-9

C22H21ClN2O4S

444.93

GSK-1605786;维塞诺;CCX282-B;Traficet-EN

DMSO:22.25 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years