A CXCR3 antagonist
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CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1 It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50 = 0.06 µM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 µM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50 = ~100 nM).
1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonistsBioorg. Med. Chem. Lett.16(1)200-203(2006)
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