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Vercirnon sodium

Names

[ CAS No. ]:
886214-18-2

[ Name ]:
Vercirnon sodium

[Synonym ]:
UNII-9NQF0M8R0M
Benzenesulfonamide,N-(4-chloro-2-((1-oxido-4-pyridinyl)carbonyl)phenyl)-4-(1,1-dimethylethyl)-,sodium salt
Vercirnon sodium [USAN]
N-(4-Chloro-2-((1-oxidopyridin-4-yl)carbonyl)phenyl)-4-(1,1-dimethylethyl) benzenesulfonamide,sodium salt
Vercirnon sodium

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CCR
Research Areas >> Endocrinology
Signaling Pathways >> Immunology/Inflammation >> CCR
Research Areas >> Inflammation/Immunology

[Target]

CCR9:10 nM (IC50)


[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]. 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.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20ClN2NaO4S

[ Molecular Weight ]:
466.91300

[ Exact Mass ]:
466.07300

[ PSA ]:
103.40000

[ LogP ]:
6.15740

Related Compounds