CCR

Aplaviroc is a CCR5 entry inhibitor developed for the treatment of HIV infection.

Cenicriviroc is an experimental drug candidate for the treatment of HIV infection.Cenicriviroc is an inhibitor of CCR2 and CCR5 receptors, allowing it to function as an entry inhibitor which prevents the virus from entering into a human cell.

Cenicriviroc, also known as TAK-652 and TBR-652, is an inhibitor of CCR2 and CCR5 receptors, allowing it to function as an entry inhibitor which prevents the virus from entering into a human cell. CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base)

ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations.

R243 is an inhibitor of CCR8 signaling and chemotaxis.

AZD2098 is a potent and selective CCR4 inhibitor with pIC₅₀ values of 7.8–8.0 across human, rat, mouse, and dog. It is commonly used in asthma research to study CCR4-mediated inflammatory pathways.

DAPTA is a synthetic peptide that acts as a selective inhibitor of the CCR5 receptor. By blocking CCR5, DAPTA interferes with viral entry into host cells, exhibiting significant anti-HIV activity. This compound is valuable for research in virology and the development of therapeutic strategies against HIV.

NSC177365 is a potent CcrM inhibitor that acts by competitively disrupting DNA binding. It demonstrates significant antibacterial activity, displaying IC50 values of 2.3 μM and 14.6 μM against C. crescentus and M. lincolnii, respectively. Furthermore, NSC177365 has potential applications in reversing neurodegenerative disorders and shows promise as an anticancer agent, making it a valuable tool for chemical research.

CCR6 Inhibitor 1 is a highly selective inhibitor of the CCR6 receptor, demonstrating IC50 values of 0.45 nM for monkey CCR6 and 6 nM for human CCR6, while exhibiting minimal activity against human CCR1 and CCR7. This inhibitor effectively prevents ERK phosphorylation, making it a valuable tool in the study of signaling pathways. CCR6 Inhibitor 1 is employed in research focused on autoimmune diseases and cancer, facilitating insights into therapeutic strategies targeting CCR6-related pathways.

Zelnecirnon is an orally active CCR4 inhibitor that effectively blocks the recruitment of Th2 inflammatory immune cells to inflamed tissues. This compound exhibits potent anti-inflammatory activity, making it valuable in researching allergic inflammation associated with conditions such as atopic dermatitis and asthma. Zelnecirnon serves as a critical tool for understanding and developing therapeutic strategies in inflammatory diseases.

Ilacirnon is a potent CCR2 antagonist that specifically targets the C-C chemokine receptor type 2 (CCR2). This compound exhibits significant inhibitory activity, making it valuable in research focused on inflammatory diseases and immune response modulation. Ilacirnon can be utilized in studies exploring the role of CCR2 in various pathophysiological conditions, including atherosclerosis and chronic kidney disease.

ALK4290 is a potent, orally active inhibitor of CCR3, exhibiting a Ki of 3.2 nM for human CCR3. Its biological activity positions ALK4290 as a valuable tool for research into neovascular age-related macular degeneration and Parkinsonism. This compound may help elucidate the role of CCR3 in these diseases, facilitating the development of targeted therapeutic strategies.

JNJ-41443532 is a selective antagonist of the human CCR2 receptor, exhibiting an IC50 of 37 nM for binding and demonstrating potent functional antagonism with an IC50 of 30 nM in chemotaxis assays. This compound shows a Ki value of 9.6 µM for murine CCR2 binding. JNJ-41443532 is suitable for research into inflammatory diseases and related inflammatory pathways.

ALK4290 dihydrochloride is a potent inhibitor of the CCR3 receptor, exhibiting a Ki value of 3.2 nM for human CCR3. This compound demonstrates significant potential for modulating immune responses, making it a valuable tool in the study of neovascular age-related macular degeneration and Parkinson's disease. Researchers can utilize ALK4290 to investigate its effects on CCR3-related signaling pathways and its implications in various pathological conditions.

ECL1i is an allosteric inhibitor targeting the CCR2 receptor. It selectively disrupts CCL2/CCR2-mediated chemotaxis, thereby impeding the recruitment of CCR2-positive cells. ECL1i has demonstrated efficacy in attenuating disease progression in models of experimental autoimmune encephalomyelitis, making it a valuable tool for studying autoimmune disease mechanisms and potential therapeutic interventions.

BX-513 is a potent and selective antagonist of the CCR1 receptor. It effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with inhibition constants (Ki) of 40 nM and 60 nM, respectively. BX-513 demonstrates the ability to suppress MIP-1α-induced extracellular acidification, as well as MIP-1α- and RANTES-induced intracellular calcium mobilization and peripheral blood mononuclear cell migration. This compound is applicable in research focusing on autoimmune diseases such as rheumatoid arthritis and multiple sclerosis.

DOTA-ECL1i is a CCR2 inhibitor conjugated with DOTA, designed for use in positron emission tomography (PET) imaging. When radiolabeled with 68Ga, DOTA-ECL1i provides a specific PET tracer that targets CCR2 expression in various pathological conditions. This compound is applicable in research focused on pulmonary fibrosis, cardiac injury, abdominal aortic aneurysm inflammation, atherosclerosis, and cancers of the head, neck, and pancreas.

CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial.

CMPD167 is a selective CCR5 inhibitor that exerts its antiviral effects by blocking the CCR5 receptor, which is critical for the entry of certain viruses into host cells. This compound demonstrates potent antiviral activity in vitro, making it a valuable tool for research on viral infections, particularly in studies related to HIV. CMPD167 can facilitate investigations into CCR5-related pathways and the development of therapeutic strategies targeting viral entry mechanisms.

CB-0821 is a high-affinity CCR5 inhibitor with a Ki value of 0.04 nM. It effectively binds to the hydrophobic pocket of the CCR5 protein, disrupting the interactions between viral proteins and CCR5, which inhibits viral entry into cells. This compound is poised for use in anti-HIV research applications, facilitating studies on viral tropism and potential therapeutic strategies.