cc chemokine receptor

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).

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.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.

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

MK-0812 Succinate is an effective and selective CCR2 antagonist. It also has a high affinity at CCR2.

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.

Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

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

R243 is CCR8 signaling and chemotaxis inhibitor.

AZD-4818 (CCR1 antagonist) is a chemokine CCR1 antagonist for the treatment of chronic obstructive pulmonary disease.

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

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

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.

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.

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