RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.

CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.

ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.

WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

Vicriviroc Malate is a potent CKR-5 (CCR5) antagonist with IC50 of 0.91 nM.

RS 102895 hydrochloride is a chemokine receptor CCR2 antagonist.

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

MSX-122 is a n orally bioavailable inhibitor of CXCR4 with potential antineoplastic and antiviral activities.

BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.

AMD3465 is a Potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100 (Cat.No. 3299). Inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist (human IC50=3 nM; rat IC50=11 nM; mice IC50=81 nM).

SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM.

ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.

CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer with an IC50 value of 6.9 nM against CXCR4-specific antagonist peptide, TN14003. CXCR4 probe 1 has potential to be used as CXCR4-specific imaging probe to diagnose and monitor the prognosis of inflammatory diseases, CXCR4-positive tumors, and metastatic cancers.

MSX-130 is CXCR4 Antagonist.

NSC-23026, also known as MSX-127, is a CXCR4 receptor modulator.

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Reparixin(DF 1681Y) is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation, which has been shown to attenuate inflammatory responses in various injury models.

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.

Vercirnon (GSK1605786A, CCX282-B) is a potent, selective, orally bioavailable antagonist of CCR9, inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 of 5.4 and 3.4 nM, respectively.Vercirnon (GSK1605786A, CCX282-B) displays high selectivity for CCR9 over CCR1-12 and CX3CR1-7 (IC50>10 uM).Vercirnon (GSK1605786A, 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.CCX282-B also inhibited 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 TNF(ΔARE) mice.

RS-1748 is a highly potent, selective, orallu active CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 59.9 nM.RS-1748 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b. dose-dependently inhibited 50 nM CCL22-induced [Ca2+]i mobilization with IC50 of 28.3 nM, inhibited the binding of [35S]GTPgS to human CCR4-expressing CHO cells with IC50 of 18.4 nM.Orally administered RS-1748 (30 mg/kg) significantly lowered the total cell numbers and the eosinophils numbers in ovalbumin-sensitized guinea pigs.

RS-1269 is a highly potent, selective CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 binding with IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells with IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo.

Lazucirnon (KST4290, ALK4290) is a small molecule, orally active inhibitor against CCR3, the natural receptor for chemokine eotaxin, decreases inflammatory cytokines in preclinical models.Lazucirnon (KST4290, ALK4290) blocks eotaxin from binding to its G-protein coupled receptor (GPCR) CCR3.CCR3 plays an important modulatory role in inflammation, immune cell recruitment, and neovascularization, processes important for the pathogenesis of wet age-related macular degeneration (wet AMD) and other neurological and immunological diseases.

IS811 is a potent, selective CCR3 antagonist with IC50 of 2.0 nM, potently inhibits chemotaxis with EC50 of 19 nM.IS811 displays >100-fold selectivity over 5-HT2a, DAT and NET.IS811 (0-20 mg/kg) dose-dependently inhibited eotaxin-induced eosinophil influx to the lung in vivo.

HF50731 (HF-50731) is a novel potent, selective CXCR4 antagonist with Ki of 19.8 nM in the CXCR4 competitive binding assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288.

GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively; does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM); produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in cell-based functional assays; demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1.

GSK-2239633 is a potent, selective, allosteric CCR4 antagonist with pIC50 of 7.96; also inhibits TARC-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with pA2 of 7.1.