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Cat. No. Product Name CAS No. Information



LIT-927 (LIT927) is the first selective, locally and orally active CXCL12 neutraligand with Ki of 267 nM for CXCL12-TR binding inhibition; displays excellent selectivity over other chemokines (CCL17, CCL22, CCL5 and CCL2), inhibits the increase in intracellular calcium concentration in EGFP-CXCR4+HEK cells in response to CXCL12 at 10 uM, has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or by CCL2 on EGFP-CCR2+HEK cells; reduces eosinophil recruitment in murine model of allergic airway hypereosinophilia.


CCR6 inhibitor 35

CCR6 inhibitor 35 is a potent and selective CCR6 inhibitor with IC50 of 6.0 nM (hCCR6); exhibits potent activity in the migration assay as well as the Gi signal assay with IC50 of <30 nM and 6 nM in human CCR6-transfected CHO cells, respectively, and displays high human CCR6 selectivity over human CCR1 and CCR7; potently inhibits CCR6-dependent cell migration and the increase in ERK phosphorylation in human primary cells.




AZ084 (AZ-084) is a potent, selective, allosteric, orally available CCR8 antagonist with Ki of 0.9 nM; demonstrates excellent selectivity in a panel of 141 kinases and receptors, also shows no binding activity at 10 uM towards any of the other chemokine receptors; demonstrates excellent selectivity, high metabolic stability in vitro and an attractive in vivo PK profile with a long half-life in rats; inhibits dendritic cell, T cell and eosinophil migration.




Elubrixin (SB-656933;GSK-656933) is a potent, selective, competitive and reversible CXCR2 antagonist; inhibits CXCL1-induced CD11b up-regulation on PMNs in an in vitro whole blood assay and to be active in in vivo rodent inhalation challenge models of airway inflammation that used endotoxin and ozone to induce airway neutrophilia.


Phase 2 Discontinued


ML 604086


ML 604086 (ML604086) is a potent, selective CCR8 inhibitor that inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations with IC50 of 1.3 uM and 1.0 uM respectively in cellular assays; displays high selectvity against a panel of 40 GPCRs, only moderately inhibits 5HT1a (30% at 10 uM).




Aplaviroc (GSK-873140, GW 873140, AK-602, ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6; blocks the calcium response effects of CCR5 activation by CCL5, and potently blocks in vitro the infection of R5-tropic HIV-1 (R5-HIV-1) at subnanomolar IC50.

HIV Infection

Phase 3 Discontinued


AZD 2098


AZD2098 is a potent, selective, orally bioavailable CCR4 receptor antagonist with pIC50 of 7.8 for hCCR4, pIC50 of 8.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.3; exhibits anti-inflammatory effects in Brown-Norway rats sensitized to ovalbumin.


Phase 1 Clinical

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