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Vercirnon Chemical Structure
|Product name: Vercirnon|
|Cat. No.: HY-15724|
Vercirnon is a highly potent antagonist of CCR9, which has been implicated in the aetiology of inflammatory bowel diseases such as Crohn's disease.
IC50 value: <7 nM (Molt-4 cells, CCR9 transfected cell, primary derived human T cells, and murine and rat thymocytes)
in vitro: CCX282-B inhibits CCR9 mediated chemotaxis to CCL25 (IC50 <7 nM), measured in the Molt-4 cells, CCR9 transfected cell lines, primary derived human T cells, and murine and rat thymocytes. CCX282-B inhibits CCR9-mediated Ca2+mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively.. CCX282-B inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. 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. 
in vivo: CCX282-B also inhibits 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 TNFΔARE mice. 
|M.Wt||444.93||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.2475 mL||11.2377 mL||22.4754 mL|
|5 mM||0.4495 mL||2.2475 mL||4.4951 mL|
|10 mM||0.2248 mL||1.1238 mL||2.2475 mL|
. 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):61-6.
. Haberer LJ, et al. Effects of vercirnon on the activity of CYP3A4, CYP2C19 and CYP2C8 enzymes and BCRP and OATP1B1 transporters using probe substrates. Eur J Clin Pharmacol. 2014 Jan;70(1):37-45.
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