Catalog No.
Product Name
Application
Product Information
Citations
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CCR3 Inhibitor
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. -
CCR2 Inhibitor
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. -
CCR2 Antagonists
CCR2-RA is an allosteric antagonist of the chemokine (C-C motif) receptor 2 (CCR2). This compound selectively inhibits CCR2 signaling, making it a valuable tool in cancer research to explore the role of chemokine receptors in tumor progression and metastasis. Its application extends to investigating the modulation of immune responses in the tumor microenvironment. -
CCR1 Antagonist
BAY-3153 is a selective antagonist of the C-C motif chemokine receptor 1 (CCR1), with human IC50 values of 3 nM, rat IC50 of 11 nM, and mouse IC50 of 81 nM. This compound serves as a valuable tool for investigating the role of CCR1 in various biological processes, including inflammation and immune response modulation. Its specificity and potency make it suitable for research applications involving chemokine signaling and receptor activity. -
CCR8 Antagonist
SB-649701 is a potent antagonist of the human CCR8 receptor, exhibiting a pIC50 of 7.7. This compound is primarily utilized in research related to asthma, providing insights into inflammatory pathways and the role of CCR8 in immune responses. Its mechanism of action makes it valuable for exploring therapeutic strategies targeting airway hyperreactivity and allergic conditions. -
CCR2 Antagonist
BMS-741672 is a selective orally active antagonist of the CCR2 receptor, exhibiting an IC50 of 1.1 nM. This compound demonstrates over 700-fold selectivity for CCR2 compared to CCR5, making it a valuable tool for investigating the role of CCR2 in inflammatory processes. BMS-741672 has potential applications in studies of immune responses and related pathologies, contributing to the understanding of therapeutic strategies targeting chemokine signaling pathways. -
CCR3 Agonist
CH0076989 is a selective agonist of the CCR3 receptor that activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimeric receptor lacking the CCR3 amino-terminus. This compound exhibits a direct interaction with the transmembrane helices of CCR3; activity is abolished by mutations of key residues Y41, Y113, and E287. CH0076989 is ideal for research into inflammation and allergic diseases, including asthma, making it a valuable tool for understanding these pathological conditions. -
CCR2 Antagonist
RO5234444 is an orally active CCR2 antagonist with an IC50 of 22 nM for human CCR2 and 161 nM for mouse CCR2. This compound demonstrates significant biological activity by alleviating glomerulosclerosis, reducing albuminuria, and improving glomerular filtration rate (GFR) in the uninephrectomized type 2 diabetic db/db mouse model. RO5234444 serves as an essential tool for the investigation of type 2 diabetic nephropathy. -
CCR3 Antagonist
YM-344031 is a potent orally active antagonist targeting the CCR3 chemokine receptor. It effectively inhibits the binding of Eotaxin-1 and RANTES to CCR3 with IC50 values of 3.0 nM and 16.3 nM, respectively. This compound also reduces ligand-induced increases in intracellular calcium levels and chemotactic responses. Additionally, YM-344031 demonstrates the ability to ameliorate eotaxin-1-induced morphological changes in eosinophils from macaque blood and mitigates allergic skin responses in murine models, making it a valuable tool for research in allergic and inflammatory conditions. -
CCR1 Antagonist
CCR1 antagonist 12 is a selective antagonist of the CCR1 receptor, exhibiting an IC50 of 3 nM for human CCR1. This compound effectively inhibits CCL3-induced transwell chemotaxis, with an IC50 of 0.009 µM, making it a valuable tool for studying chemokine-mediated signaling pathways. Additionally, CCR1 antagonist 12 demonstrates favorable pharmacokinetic properties in rat models, supporting its potential use in preclinical research. -
CCR3 Antagonist
Maceneolignan H is a selective CCR3 antagonist, with an EC50 value of 1.4 μM. Isolated from the arils of Myristica fragrans, this neolignane compound demonstrates significant potential in the study of allergic diseases. Its ability to inhibit CCR3 suggests applications in researching therapeutic strategies for conditions mediated by this receptor. -
Ligand for CCR2
CCR2 ligand-1 is a potent ligand for the chemokine receptor CCR2, playing a crucial role in mediating inflammatory responses. This compound is valuable for studying CCR2 signaling pathways and its implications in diseases such as cancer and rheumatoid arthritis. Additionally, CCR2 ligand-1 can be utilized in the synthesis of LUF7996 when conjugated with Linker PIN1 degrader-3 and E3 ligase ligand Thalidomide 4-fluoride, facilitating research in targeted protein degradation. -
CCR3 Antagonist
BMS-639623 is a highly potent and orally bioavailable antagonist of the chemokine receptor CCR3, exhibiting an IC50 value of 0.3 nM. This compound demonstrates exceptional inhibitory activity against eosinophil chemotaxis, with an IC50 of 38 pM. BMS-639623 is primarily utilized in research focused on asthma and related inflammatory conditions. -
CCR3 Antagonist
CCR3 Antagonist 2 is a selective antagonist of the CCR3 receptor, a chemokine receptor involved in mediating inflammatory responses. This compound is particularly useful for research applications related to inflammatory and allergic conditions, including obstructive airways diseases. By interfering with CCR3 signaling, it allows for the exploration of therapeutic strategies aimed at modulating immune responses associated with these pathologies. -
CCR Antagonist
RAP-103 is a potent orally active CCR antagonist that targets the CCR pathway to provide synaptic protection. It effectively inhibits and reverses cytoskeletal alterations induced by PrPC/NOX signaling. RAP-103 is particularly relevant for research applications focused on Alzheimer's disease, offering insights into neuroprotective mechanisms and potential therapeutic strategies. -
CCR1 Inhibitor
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. -
CCR2/CCR5 Antagonist
PF-4178903 is a potent dual antagonist of the chemokine receptors CCR2 and CCR5, exhibiting IC50 values of 3 nM and 5.3 nM, respectively. This orally active compound is valuable in the study of chronic inflammatory conditions and autoimmune diseases, providing insights into the modulation of immune responses. Its dual targeting capability makes PF-4178903 a significant tool for exploring therapeutic avenues in related research applications. -
CCR8 Agonist
LMD-584 is a selective agonist of CCR8, a chemokine receptor involved in immune responses and inflammation. This compound demonstrates significant biological activity in modulating CCR8 signaling pathways, making it a valuable tool for research applications focused on immune cell trafficking and related pathologies. LMD-584 may aid in understanding the role of CCR8 in various diseases, including cancer and autoimmune disorders. -
CCR5 Modulator
CCR5 modulator-1 is a selective modulator of the CCR5 chemokine receptor. This compound plays a significant role in the regulation of inflammatory processes and can be applied in research aimed at understanding various inflammatory diseases. Its use may provide insights into therapeutic strategies targeting CCR5-related pathways. -
Anti-CCR2 Antibody
Minokitug is a humanized monoclonal antibody that specifically targets the CCR2 protein. It exhibits significant biological activity by inhibiting CCR2-mediated signaling pathways, making it a valuable tool for studying inflammatory processes. This reagent is particularly relevant in research focused on refractory or relapsed ulcerative colitis, aiding in the understanding of the disease's pathophysiology and potential therapeutic interventions. -
CCR2 PROTAC Degrader
LUF7996 is a potent CCR2 PROTAC degrader that selectively targets and degrades CCR2 with a DC50 value of 2.6 μM. This compound effectively engages with the E3 ligase cereblon, promoting sustained and concentration-dependent degradation of CCR2 via the lysosomal pathway. LUF7996 is particularly valuable for research applications involving the inhibition of monocyte migration in vitro, facilitating studies in inflammation and immune response modulation. -
CCR1 Antagonist
cis-J-113863 is a competitive antagonist of chemokine receptor 1 (CCR1) that exhibits potent inhibitory effects, with IC50 values of 0.9 nM for human CCR1 and 5.8 nM for mouse CCR1. This compound is valuable for research in inflammation, immune response, and related therapeutic areas, facilitating the investigation of CCR1's role in various biological processes and disease models. -
CCR1 Antagonist
CCR1 antagonist 13 is a selective antagonist of the CCR1 chemokine receptor. This small molecule inhibitor effectively disrupts CCR1 signaling, making it a valuable tool for investigating the roles of CCR1 in inflammatory responses and immune cell migration. Its applications extend to research on autoimmune diseases, chronic inflammatory conditions, and the modulation of chemokine-mediated pathways. -
CCR2 Inhibitor-DOTA Conjugate
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. -
CCR6/CXCR2 Antagonist
SQA1 is a squaramide derivative that functions as a CCR6 and CXCR2 antagonist, displaying a dissociation constant (Kd) of 250 nM. It effectively occupies the intracellular pocket, overlapping with the G protein binding site, which helps stabilize the closed conformation of the receptor. This compound is useful in research applications targeting chemokine receptor signaling pathways and their roles in inflammatory responses and immune cell trafficking. -
CCR2 Antagonist
CCR2 Antagonist 6 is a potent CCR2 antagonist with a Ki value of 0.215 μM for CCR2 and 0.174 μM for human CCR2B. This compound exhibits significant biological activity by inhibiting the CCR2 receptor, making it a valuable tool for studying inflammatory processes and autoimmune diseases. Its specificity and efficacy contribute to the understanding of CCR2-related pathways in various pathophysiological conditions. -
CCR5 Antagonist
CCR5 antagonist 5 is an effective CCR5 antagonist that targets the CCR5 receptor, playing a critical role in modulating immune response and inflammation. This compound is particularly valuable for research applications focused on HIV infection and other viral pathogens, offering insights into therapeutic strategies for immunological disorders and viral disease management. -
CCR9 Modulator
CCR9 modulator-1 is a selective modulator of the chemokine receptor CCR9, primarily involved in T-cell trafficking and immune response regulation. This compound demonstrates significant potential in influencing CCR9-mediated immune pathways, making it a valuable tool for the study of inflammatory diseases such as Crohn's disease and other gastrointestinal disorders. Researchers can utilize CCR9 modulator-1 to explore therapeutic strategies targeting CCR9 in various immunological contexts. -
CCR1/CCR3 Antagonist
trans-J-113863 is a potent antagonist of the CCR1 and CCR3 chemokine receptors. It effectively inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, exhibiting IC50 values of 9.57 nM and 93.8 nM, respectively. This compound serves as a valuable tool for research focused on inflammation and immune responses, offering insights into the roles of these receptors in various biological contexts. -
CCR8 Antagonist
CCR8 antagonist 3 is a selective antagonist of the CCR8 receptor, exhibiting an IC50 value of 0.062 µM. This compound demonstrates stability in human microsomes, making it suitable for various in vitro studies. Its potential applications include exploring mechanisms of immune response modulation and investigating therapeutic strategies for inflammatory diseases and cancer. -
CCR5/CXCR3 Inhibitor
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. -
CCR1 Antagonist
CP-865569 is a potent CCR1 antagonist, specifically designed to inhibit the activity of the CCR1 chemokine receptor. This compound demonstrates potential therapeutic effects in the modulation of inflammatory responses, making it valuable for research into inflammatory and autoimmune diseases, including rheumatoid arthritis and multiple sclerosis. Its ability to selectively target CCR1 makes CP-865569 an important tool for investigating the roles of chemokines in disease pathology and therapeutic intervention. -
CCR1 Antagonist
BMS-457 is a potent and selective antagonist of the chemokine receptor CCR1. This compound demonstrates significant biological activity in modulating inflammatory pathways and is primarily utilized in research applications related to rheumatoid arthritis. Its ability to inhibit CCR1 makes it a valuable tool for studying the role of chemokines in autoimmune disorders. -
CCR5 Antagonist
SCH 350581 is a CCR5 antagonist that effectively inhibits HIV-1 replication. By obstructing viral entry into host cells and preventing the binding of the gp120 protein to primary lymphocytes, SCH 350581 plays a critical role in studying HIV-1 pathogenesis and potential therapeutic interventions. This compound is valuable for research applications focused on antiviral drug development and the mechanisms of HIV entry. -
CCR8 Antagonist
AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications. -
CXCR Antagonist
ACT-1004-1239 is a selective antagonist of the CXCR7 receptor, exhibiting a potent inhibitory effect with an IC50 value of 3.2 nM. This compound is primarily utilized in research focused on chemokine signaling pathways and is relevant in studies investigating disorders related to the immune system and cancer. Its oral bioactivity makes it an attractive candidate for in vivo investigations targeting CXCR7-mediated pathways. -
CXCR4 Receptor Agonist
NUCC-390 dihydrochloride is a selective small-molecule agonist of the CXCR4 receptor. It promotes the internalization of CXCR4 receptors and exhibits effects that are opposite to those of conventional CXCR4 antagonists. This compound has demonstrated the potential to enhance nerve recovery following neurodegeneration in vivo, making it a valuable tool for research in neurobiology and therapeutic applications targeting nerve regeneration. -
CXCR3 Antagonist
ACT-777991 is a selective antagonist of the CXCR3 receptor, demonstrating oral bioavailability. This compound effectively inhibits the migration of activated T cells in response to CXCL11, making it a useful tool for studying immune responses and inflammatory conditions. Its stability in microsomes and hepatocytes across various animal models further supports its potential applications in pharmacological research related to autoimmune diseases and cancer immunotherapy. -
ACKR7 Agonist
VUF11207 fumarate is a selective agonist of the ACKR7 receptor (formerly known as CXCR7). This compound effectively inhibits CXCL12-induced osteoclastogenesis and bone resorption by preventing ERK phosphorylation. VUF11207 fumarate is valuable for research targeting bone metabolism and related pathologies, making it a key tool for studying the role of ACKR7 in bone homeostasis and signaling pathways. -
CXCR3 Agonist
PS372424 hydrochloride is a selective agonist of the CXCR3 receptor, a key player in immune response modulation. This compound exhibits anti-inflammatory properties by inhibiting human T-cell migration, making it valuable for research into inflammatory diseases, particularly in models of arthritic inflammation. Its ability to target CXCR3 offers insight into the therapeutic potential for treating conditions characterized by dysregulated T-cell activity. -
CXCR2/1 Antagonist
SX-517 is a dual antagonist of CXCR2 and CXCR1, featuring a boronic acid structure. It effectively inhibits CXCL1-induced calcium flux with an IC50 of 38 nM and disrupts CXCL8-induced [(35)S]GTPγS binding, showing an IC50 of 60 nM, while also preventing ERK1/2 phosphorylation. This compound demonstrates significant anti-inflammatory properties in both humanized polymorphonuclear (PMN) cells and murine models, making it a valuable tool for research into inflammation-related pathways. -
Isomer
(Rac)-Reparixin is an isomer of Reparixin and serves as a useful experimental control in research settings. Reparixin functions as a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2, exhibiting inhibitory constants (IC50) of 1 nM and 100 nM, respectively. This compound is valuable for studies focusing on inflammation, cancer biology, and other pathways mediated by chemokine signaling. -
Dual CXCR1/2 Antagonist
Ladarixin sodium is a dual antagonist of CXCR1 and CXCR2, exhibiting an allosteric non-competitive mechanism. This compound demonstrates significant anti-inflammatory activity, making it relevant for research in chronic obstructive pulmonary disease (COPD) and asthma. Its ability to inhibit CXCR1 and CXCR2 pathways positions Ladarixin sodium as a valuable tool for exploring therapeutic strategies in respiratory inflammatory conditions. -
CXCR2 Antagonist
CXCR2-IN-2 is a selective antagonist of the CXCR2 receptor, demonstrating high potency with an IC50 of 5.2 nM in a β-arrestin assay and 1 nM in the CXCR2 Tango assay. This compound exhibits significant selectivity, being approximately 730-fold more selective for CXCR2 over CXCR1 and greater than 1900-fold over other chemokine receptors. Additionally, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood with an IC50 of 0.04 μM, making it a valuable tool for research into inflammatory processes and associated therapeutic applications. -
CXCR Modulator
CXCR7 modulator 2 is a selective modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), exhibiting an affinity with a Ki value of 13 nM. This compound plays a critical role in research applications focusing on chemokine signaling pathways and their involvement in various physiological and pathological processes. It is particularly useful in studies related to cancer metastasis, inflammation, and cardiovascular diseases, making it a valuable tool for understanding CXCR7's biological functions. -
CXCR2 Antagonist
CXCR2 antagonist 8 is a potent and selective antagonist of the CXCR2 receptor, involved in inflammatory responses and immune cell migration. This compound has demonstrated significant activity in models of insulin resistance, making it a valuable tool for investigating metabolic disorders and related signaling pathways. Researchers can utilize CXCR2 antagonist 8 for studies aimed at elucidating the role of CXCR2 in various disease states. -
CXCR4 Receptor Agonist
NUCC-390 is a selective small-molecule agonist of the CXCR4 receptor. This compound induces internalization of CXCR4 receptors, thereby modulating signaling pathways distinct from antagonists. Research indicates that NUCC-390 promotes functional recovery of nerve tissue following neurodegeneration, making it a valuable tool for applications related to neurobiology and regenerative medicine. -
CXCR4 Antagonist
EPI-X4 is a selective antagonist of the C-X-C motif chemokine receptor 4 (CXCR4), exhibiting an IC50 of 8.6 μM. This compound effectively inhibits CXCL12-mediated signaling and reduces chemokine-driven migration and invasion in leukemia cells. Additionally, EPI-X4 demonstrates anti-inflammatory properties in mouse models and displays antiviral activity against CXCR4-tropic HIV, making it a valuable tool for research in cancer, inflammation, and virology. -
CXCR3 Antagonist
ACT-660602 is an orally active antagonist of the chemokine receptor CXCR3, demonstrating an IC50 value of 204 nM. This compound effectively inhibits T-cell migration, making it a valuable tool in the study of immune response. ACT-660602 has shown efficacy in models of acute lung injury and is relevant for research focused on autoimmune diseases and related inflammatory conditions. -
CXCR2 Antagonist
SB-332235 is a potent, orally active nonpeptide antagonist of the chemokine receptor CXCR2, exhibiting an IC50 of 7.7 nM and demonstrating 285-fold selectivity for CXCR2 over CXCR1. This compound has been shown to effectively inhibit both acute and chronic models of arthritis in rabbits. Additionally, SB-332235 reduces the viability of acute myeloid leukemia (AML) cells, indicating its potential utility in cancer research and therapeutic applications for inflammatory diseases.
