human cxcr3

SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.

CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It 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)

PS372424 is a specific agonist of human CXCR3, with anti-inflammatory activity.

PS372424 is a specific agonist of human CXCR3. It has been shown to induce phosphorylation of ERK and block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice.

ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4 5 and CXCR3 4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.

(R)-SCH 546738, the R-isomer of SCH 546738, is a non-competitive, orally active antagonist targeting the CXCR3 receptor, exhibiting a K_i of 0.4 nM for the human CXCR3 receptor.