Vercirnon sodium

Description: Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells with IC50 values of 5.4 nM and 3.4 nM, respectively. Vercirnon sodium demonstrates high selectivity, showing IC50 values exceeding 10 µM for CCR1-12 and CX3CR1-7 receptors. It also inhibits CCL25-directed chemotaxis in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively. Target: Others. Smiles: [Na].CC(C)(C)c1ccc(cc1)S(=O)(=O)Nc1ccc(Cl)cc1C(=O)c1ccn(=O)cc1. References: 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.