Vercirnon

• CAT Number: I004622
• CAS Number: 698394-73-9
• Molecular Formula: C22H21ClN2O4S
• Molecular Weight: 444.93
• Purity: ≥95%
• Target: CCR9
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: <7 nM (Molt-4 cells, CCR9 transfected cell, primary derived human T cells, and murine and rat thymocytes)

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)Target: CCR9in 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.[1] 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. [2]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. [2]

Reference

1:Randomised clinical trial: vercirnon, an oral CCR9 antagonist, vs. placebo as induction therapy in active Crohn/’s disease. Feagan BG, Sandborn WJ, D/’Haens G, Lee SD, Allez M, Fedorak RN, Seidler U, Vermeire S, Lawrance IC, Maroney AC, Jurgensen CH, Heath A, Chang DJ.Aliment Pharmacol Ther. 2015 Nov;42(10):1170-81. doi: 10.1111/apt.13398. Epub 2015 Sep 23. PMID: 26400458 Free Article2:Effects of vercirnon on the activity of CYP3A4, CYP2C19 and CYP2C8 enzymes and BCRP and OATP1B1 transporters using probe substrates. Haberer LJ, McSherry I, Cargill A, McCarthy L.Eur J Clin Pharmacol. 2014 Jan;70(1):37-45. doi: 10.1007/s00228-013-1592-7. Epub 2013 Oct 8. PMID: 24100471 Free PMC Article3:Single-Dose Pharmacokinetics of the CCR9 Receptor Antagonist Vercirnon in Healthy US and Japanese Subjects. Haberer LJ, Hacquoil K, Ino H, Sakamoto T, Kanemoto N, McSherry I, Hirama T.Clin Pharmacol Drug Dev. 2013 Oct;2(4):387-93. doi: 10.1002/cpdd.41. Epub 2013 Aug 11. PMID: 27121943 4:Vercirnon for the treatment of Crohn/’s disease. Arseneau KO, Cominelli F.Expert Opin Investig Drugs. 2013 Jul;22(7):907-13. doi: 10.1517/13543784.2013.795946. Epub 2013 Apr 30. Review. PMID: 23627683