ccr

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.

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.

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

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.

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

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

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

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

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.

CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 μM. CCR4 antagonist 3-1 inhibits the binding of radiolabeled [125I]TARC and macrophage-derived chemokine ( MDC) to CEM cell surface and inhibits TARC-mediated CEM cell migration in vitro with an IC50 value of 6.4 μM. CCR4 antagonist 3 inhibited the binding of radiolabeled [125I]TARC and macrophage-derived chemokine (MDC) to the CCR4 receptor on the surface of CEM cells and inhibited TARC-mediated migration of CEM cells in vitro with an IC50 value of 6.4 μM.

CCR8 antagonist 1 is an antagonist of C-C Motif Chemokine Receptor 8 (CCR8) with a Ki value of 1.6 nM.

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.

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

CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).

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

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

CCR5 antagonist 1, derived from WO 2004054974 A2, is a CCR5 antagonist that inhibits HIV replication.

CCR1 antagonist 9 is an effective and selective CCR1 antagonist (IC50: 6.8 nM in calcium flux assay).

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

CCR2 antagonist 1 is a high-affinity antagonist of CCR2 with a Ki of 2.4 nM and a long residence time.

CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).

CCR6 inhibitor 1 is an effective and selective inhibitor of CCR6 (IC50 of monkey and human CCR6 was 0.45 nM and 6 nM, respectively). CCR6 is associated with both autoimmune and non-autoimmune diseases, so CCR6 inhibitor 1 is useful for in vitro and in vivo pathophysiology studies as a small molecule inhibitor of CCR6.

CCR6 antagonist 1, a chemical compound acting as a CCR6 antagonist, effectively inhibits the CCL20 CCR6 axis. Its utility lies in research focused on autoimmune-mediated inflammatory diseases, including inflammatory bowel diseases (IBDs).