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Vercirnon

Chemical Structure : Vercirnon

CAS No.: 698394-73-9

Vercirnon (GSK-1605786, CCX282-B, Traficet-EN)

Catalog No.: PC-73249Not For Human Use, Lab Use Only.

Vercirnon (GSK1605786A, CCX282-B) is a potent, selective, orally bioavailable antagonist of CCR9, inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 of 5.4 and 3.4 nM, respectively.

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Biological Activity

Vercirnon (GSK1605786A, CCX282-B) is a potent, selective, orally bioavailable antagonist of CCR9, inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 of 5.4 and 3.4 nM, respectively.
Vercirnon (GSK1605786A, CCX282-B) displays high selectivity for CCR9 over CCR1-12 and CX3CR1-7 (IC50>10 uM).
Vercirnon (GSK1605786A, CCX282-B) 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.
CCX282-B also inhibited mouse and rat CCR9-mediated chemotaxis.
Inhibition of CCR9 with CCX282-B results in normalization of Crohn's disease such as histopathology associated with the TNF(ΔARE) mice.

Physicochemical Properties

M.Wt 444.93
Formula C22H21ClN2O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

1. Walters MJ, et al. J Pharmacol Exp Ther. 2010 Oct;335(1):61-9.

2. Keshav S, et al. PLoS One. 2013;8(3):e60094.

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