ccr

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

Bindarit is a selective inhibitor of monocyte chemoattractant proteins MCP-1 CCL2, MCP-3 CCL7 and MCP-2 CCL8 with anti-inflammatory effects. Bindarit specifically inhibits p65- and p65 p50-induced MCP-1 promoter activation and has no effect on other tested activated promoters.

Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.

AZ084 is a potent, selective, allosteric, and orally active CCR8 antagonist (Ki: 0.9 nM) with potential to treat asthma.

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 binding to CCR8 on circulating T-cells.

PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.

BMS-813160 is the first dual CCR2 CCR5 antagonist to enter Clinical development for cardiovascular.

SB297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ. It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells. It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).

RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).

Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

DAPTA (Adaptavir) is an inhibitor of CCR5, shows potent anti-HIV activities.

7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

CCR-11 is a tannin-containing derivative with antimicrobial activity. CCR-11 inhibits the proliferation of B. subtilis and HeLa cells. CCR-11 inhibits bacterial proliferation and bacterial cytoplasmic division by inhibiting FtsZ assembly and GTPase activity. CCR-11 has potential anti-tumor activity and can be used to study breast cancer and pediatric myelodysplasia.

CCR3 antagonist 1 is a potent CCR3 antagonist used in researching inflammatory and immunologic diseases.

CCR8 agonist1 (Compound 2) is an activator of CCR8 and is applicable in studies related to autoimmune diseases.

CCR6 antagonist2 (Compound 20c) acts as a CCR6 antagonist with a Ki of 1.1 nM. It inhibits CCL20-induced calcium influx with an IC50 of 4.9 nM and suppresses the chemotactic migration of CCR6+ T cells with an IC50 of 190 nM.

CCR1 antagonist13 is a selective small molecule antagonist of CCR1.