Catalog No.
Product Name
Application
Product Information
Citations
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Mononuclear Cells Chemoattractant
SDF-1α (human) is a potent chemoattractant for mononuclear cells that targets the CXCR4 receptor. This cytokine plays a critical role in various biological processes, including stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis, and ventricular remodeling following myocardial infarction. SDF-1α (human) is primarily utilized in research focused on cardiovascular diseases and regenerative medicine. -
CXCR4 Antagonist
CXCR4 antagonist 5 is a potent antagonist targeting the CXCR4 receptor, exhibiting an IC50 value of 8.8 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium influx with an IC50 of 0.02 nM and blocks CXCR4/CXCL12-mediated chemotaxis. Additionally, CXCR4 antagonist 5 demonstrates favorable physicochemical properties along with a moderate safety profile in vitro, showing minimal inhibition of CYP isozymes and hERG channels. -
CXCR3 Antagonist
(R)-SCH 546738 is a selective antagonist of the CXCR3 receptor, exhibiting non-competitive inhibition with a Ki value of 0.4 nM. This compound demonstrates potent biological activity against CXCR3, making it valuable for research applications targeting inflammatory diseases and immune responses. Its oral bioavailability enhances its utility in in vivo studies, facilitating a deeper understanding of CXCR3-related signaling pathways. -
CXCR4 Antagonist
CXCR4 Antagonist 9 is a potent inhibitor of the CXCR4 receptor, exhibiting an IC50 value of 15 nM. This compound effectively suppresses CXCL12-induced increases in cytosolic calcium levels, with a notable IC50 of 1.3 nM. It is valuable for research applications focused on cell signaling pathways and the modulation of immune responses involving the CXCR4/CXCL12 axis. -
CXCR4 Antagonist
CXCR4 Antagonist 3 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 of 11 nM. This compound, a congener of TIQ15, showcases excellent properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. It is a valuable reagent for research focused on human immunodeficiency virus and related pathologies. -
Biochemical Assay Reagent
SFB-AMD3465 is a derivative of AMD3465, serving as a biochemical assay reagent. This compound functions as a positron emission tomography (PET) tracer for the chemokine receptor CXCR4 when labeled with radioactive fluorine. It is a valuable tool for exploring CXCR4-related signaling pathways and has applications in cancer research and imaging studies. -
CXCR7 Agonist
VUF11207 TFA is a potent agonist of the CXCR7 receptor, exhibiting a pKi of 8.1. This compound effectively induces the recruitment of β-arrestin2, with an EC50 value of 8.8, and facilitates the internalization of CXCR7, demonstrating an EC50 of 7.9. VUF11207 TFA is valuable for research applications focusing on CXCR7 signaling pathways and their implications in various biological processes. -
CXCR2 Inhibitor
NVP CXCR2 20 is a selective inhibitor of the CXCR2 receptor, primarily involved in modulating pain pathways. It exhibits significant analgesic and antinociceptive effects, effectively reducing mechanical and thermal hypersensitivity in rat models of chronic constriction injury (CCI). Additionally, NVP CXCR2 20 diminishes CXCL3-induced hypersensitivity in naive mice and lowers CXCL3 protein levels in the spinal cord and dorsal root ganglia of CCI-exposed rats. This compound is valuable for research into neuropathic pain and chronic obstructive pulmonary disease (COPD). -
CXCR3 Antagonist
ACT-672125 is a potent antagonist of the CXCR3 receptor, exhibiting an IC50 value of 239 nM in human blood. Additionally, it shows hERG activity with an IC50 of 18 μM. This compound is primarily utilized in research investigating autoimmune diseases, providing insights into the modulation of immune responses. -
CXCR4 Antagonist
TIQ-15 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 6 nM for CXCR4-mediated Ca2+ flux. Additionally, it demonstrates inhibition of CYP450 2D6 with an IC50 of 0.32 μM. This compound is valuable for research into CXCR4-related signaling pathways and drug metabolism. -
Inverse CXCR3 Agonist
VUF11211 is an allosteric inverse agonist of the CXCR3 receptor, exhibiting a dissociation constant (Kd) of 0.65 nM. This compound modulates CXCR3 signaling pathways, influencing immune cell migration and activation. VUF11211 is primarily used in research focused on inflammation, autoimmune diseases, and cancer immunotherapy, providing insights into the role of CXCR3 in various pathological conditions. -
Radiolabeled Peptide
Pentixather is a radiolabeled peptide that specifically targets the CXCR4 receptor. By interfering with the CXCR4/CXCL12 signaling axis, Pentixather disrupts the interaction between leukemic cells and the bone marrow microenvironment, thereby promoting the release of leukemic cells from the protective niche and increasing their sensitivity to therapeutics. This compound is valuable for research applications in acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). -
CXCR4 ligand
SDNUM04 is a ligand for the C-X-C chemokine receptor 4 (CXCR4), known for its role in cell migration and metastasis. This compound can be utilized as a tracer in tumor-targeting studies, facilitating research on cancer biology and the mechanisms of tumor progression. Additionally, SDNUM04 may serve as a valuable tool in drug discovery and development focused on CXCR4-related pathways. -
CXCR4 Modulator
CXCR4 modulator-2 is a potent antagonist of the CXCR4 receptor with an IC50 value of 1.25 nM. It demonstrates significant stability in mouse serum, with a half-life of 77.1 minutes, and showcases anti-inflammatory effects in mouse edema models. This compound is valuable for research in inflammation and immune response modulation. -
CXCR4 Antagonist
IS4 is a selective competitive antagonist of the CXCR4 receptor, exhibiting an IC50 of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. It effectively inhibits CXCL12-induced intracellular Ca2+ release and cancer cell migration by binding to CXCR4. Due to its stability in serum and low cytotoxicity, IS4 is valuable for research into the prevention of metastasis in various cancers, including breast cancer, prostate cancer, and leukemia. -
CXCR3 Antagonist
Hypoglaucin A is a CXCR3 antagonist with an IC50 value of 0.47 μM, exhibiting significant inhibitory effects on CXCR3-mediated signaling pathways. This compound is particularly relevant for research into inflammatory processes, as CXCR3 is implicated in various immune responses. Hypoglaucin A can be utilized to investigate the role of CXCR3 in inflammation-related studies and potential therapeutic applications. -
CXCR4 Antagonist
CXCR4 antagonist 8 is a selective antagonist of the CXCR4 receptor, demonstrating an IC50 of 57 nM. It effectively inhibits CXCL12-induced increases in cytosolic calcium with an IC50 value of 0.24 nM. This compound is valuable for investigating CXCL12/CXCR4-mediated cell migration and cellular signaling pathways related to various biological processes, including cancer metastasis and immune cell trafficking. -
CXCR1/CXCR2 Antagonist
SX-576 is a potent antagonist of CXCR1 and CXCR2, exhibiting IC50 values of 31 nM and 21 nM, respectively. This compound effectively inhibits neutrophil infiltration in rat models of pulmonary inflammation, making it a valuable tool for research into inflammatory diseases. SX-576 is suitable for investigations focused on the role of these chemokine receptors in pulmonary inflammation and related pathologies. -
Stable Isotope
Nicotinamide N-oxide-d4 is a deuterium-labeled derivative of Nicotinamide N-oxide, which serves as a stable isotope for analytical studies. As a notable in vivo metabolite of nicotinamide, Nicotinamide N-oxide exhibits potent and selective antagonistic activity against the CXCR2 receptor. This compound is valuable for research applications involving receptor signaling, metabolic pathways, and the study of inflammatory responses. -
CXCR Antagonist
VUF10132 is a non-peptide antagonist targeting the CXCR3 receptor, demonstrating significant anti-inflammatory activity. It effectively inhibits conditions such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has a high affinity for the human CXCR3 receptor, with a slightly lower affinity for the murine counterpart, and also exhibits inverse agonist properties, making it a valuable tool for studying CXCR3-related signaling in various inflammatory diseases. -
CXCR3 Activator
VUF11418 is an activator of the chemokine receptor CXCR3. This compound plays a significant role in modulating inflammatory responses and is valuable for studying inflammation-related pathways. VUF11418 is particularly useful in research applications focusing on immune responses and related therapeutic strategies. -
CXCL12 Inhibitor
4-Amino-D-phenylalanine is a potent CXCL12 inhibitor that targets the CXCR4 receptor. With an IC50 value of 0.1 μM, it effectively inhibits the binding of CXCL12 to its receptor. This compound is valuable for research applications focused on understanding CXCR4-related pathways and their implications in cancer, inflammation, and various other diseases. -
CXCR2 Antagonist
CXCR2 antagonist 3 is a potent inhibitor of CXC chemokine receptor 2 (CXCR2), exhibiting double-digit nanomolar potency. It effectively reduces neutrophil and myeloid-derived suppressor cell (MDSC) infiltration while promoting the infiltration of CD3+ T lymphocytes in Pan02 tumor tissues. This antagonist is valuable for research applications focusing on inflammation and tumor microenvironment remodeling. -
hKOR Activator
BAM-12P is a pro-Met-enkephalin that functions as a selective activator of the human κ-opioid receptor (hKOR), exhibiting an EC50 value of 101 nM. Additionally, BAM-12P also interacts with the CXCR7 receptor, with an EC50 of 175 nM. This compound is valuable in research applications investigating opiate receptor signaling pathways and the role of endogenous peptides in pain modulation and neurobiology. -
ACKR3 (CXCR7) Agonist
LIH383 is a selective agonist of ACKR3 (CXCR7) with an EC50 of 0.61 nM. This compound effectively promotes the recruitment of β-arrestin to ACKR3, while distinctly lacking the activation of classical G protein signaling pathways. LIH383 is useful for studies investigating the role of ACKR3 in cellular processes and its potential therapeutic applications in various diseases. -
CXCR4 Inhibitor
vMIP-II (1-21) is a selective inhibitor of the chemokine receptor CXCR4. By competing with 125I-SDF-1R for binding sites, vMIP-II (1-21) effectively disrupts CXCR4 signaling, with an IC50 value of 190 nM. This compound is useful for research applications involving the study of chemokine receptors and their role in various biological processes, such as immune response and cancer metastasis. -
CXCR4 Antagonist
BPRCX 714 is an antagonist of the CXCR4 (CXC chemokine receptor type 4), a critical receptor implicated in various cancer metastasis processes. It exhibits potential therapeutic effects by inhibiting CXCR4 signaling, making it valuable for research into hepatocellular carcinoma and other CXCR4-related malignancies. Its application in studies enhances understanding of tumor microenvironment interactions and provides insights into targeted cancer therapies. -
CXCR3 Antagonist
(±)-AMG 487 is a selective antagonist of CXC chemokine receptor 3 (CXCR3), effectively inhibiting the binding of CXCL10 and CXCL11 with IC50 values of 8.0 nM and 8.2 nM, respectively. This compound demonstrates significant potential in studying immune responses and inflammatory processes due to its ability to block CXCR3-mediated signaling. Its oral bioavailability enhances its utility in preclinical and clinical research applications targeting inflammatory diseases and cancer. -
CXCR4 Antagonist
ICT5040 is a small molecule antagonist targeting the chemokine receptor CXCR4, with an IC50 of 3.8 μM. This compound effectively inhibits CXCL12-mediated cell proliferation and migration in glioma cells, specifically U87 cells, and suppresses CXCL12-induced intracellular calcium mobilization. ICT5040 serves as a valuable tool for investigating the role of the CXCR4/CXCL12 axis in cancer research and potential therapeutic applications. -
CCR7 Antagonist
SLW131 is a potent CCR7 antagonist, demonstrating a high affinity with a Ki value of 9.85 nM. This compound effectively inhibits CCL19-induced Go protein activation with an IC50 of 29.4 μM, as well as β-arrestin2 recruitment with an IC50 of 6.0 μM. SLW131 also disrupts CCL19-induced morphological alterations in primary bone marrow-derived dendritic cells and impedes CCR7-mediated migration in mouse CD4+ T cells, making it a valuable tool for research in immune response and cell signaling pathways. -
CXCR
CX4338 is a selective inhibitor of the chemokine receptor CXCR2, targeting CXCL8-mediated pathways. This compound effectively inhibits CXCR2-mediated cell migration by suppressing β-arrestin-2 recruitment and receptor internalization while enhancing MAPK activation. CX4338 demonstrates potent inhibition of CXCL8-induced chemotaxis in CXCR2-overexpressing cells and human neutrophils. In vivo studies have shown that CX4338 significantly reduces LPS-induced neutrophil infiltration in mouse bronchoalveolar lavage fluid, highlighting its potential for research in inflammatory and immune responses. -
Inflammatory Peptide
Peptide 78 is an inflammatory peptide that functions as a chemotactic cytokine, belonging to the IL-8 or C-X-C chemokine supergene family. This 78 amino acid protein is essential for the recruitment of neutrophils to sites of inflammation, particularly in rheumatoid arthritis (RA) pathology. Its role in promoting neutrophil migration makes Peptide 78 a valuable tool for research into inflammatory diseases and immune responses. -
CXCR4 Inhibitor
TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression. -
CXCR4 Antagonist
CXCR4 antagonist 6 is a potent inhibitor of the CXCR4 receptor, displaying an IC50 value of 79 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, thereby significantly reducing CXCL12/CXCR4-mediated cell migration. Additionally, CXCR4 antagonist 6 demonstrates substantial efficacy in in vivo cancer metastasis models, making it a valuable tool for research in cancer biology and therapeutic development. -
CXCR Antagonist
CXCR4 Antagonist 2 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 47 nM. This compound effectively inhibits CXCR4-mediated signaling, making it a valuable tool for studying its role in various biological processes, including cancer metastasis, immune cell trafficking, and HIV infection. Its selective properties make it suitable for research applications aimed at understanding CXCR4 functions and developing therapeutic strategies targeting this receptor. -
CXCR4 Antagonist
KRH-1636 is a potent CXCR4 antagonist, primarily targeting the CXCR4 receptor. This compound plays a significant role in HIV-1 research by inhibiting the interaction between the virus and the CXCR4 receptor, which is crucial for viral entry into host cells. KRH-1636 serves as a valuable tool for studying the mechanisms of HIV-1 infection and for exploring therapeutic strategies aimed at disrupting CXCR4-mediated pathways. -
Drd2 Agonist
UNC9995 is a β-arrestin2-biased agonist of the dopamine receptor Drd2. This compound inhibits NLRP3 inflammasome activation by promoting the interaction between β-arrestin2 and NLRP3, thereby preventing neuronal degeneration. Furthermore, UNC9995 activates Drd2/β-arrestin2 signaling, which mitigates the transcription of inflammation-related genes induced by the JAK/STAT3 pathway. Research shows that UNC9995 enhances depressive behavior in mouse models and improves astrocyte dysfunctions, making it a valuable tool for studying neuroinflammatory processes and mood disorders. -
CXCR6 Antagonist
ML339 is a selective antagonist of the CXCR6 receptor, displaying an IC50 of 140 nM. It inhibits β-arrestin recruitment and the cAMP signaling pathway induced by CXCL16 in human CXCR6, with IC50 values of 0.3 μM and 1.4 μM, respectively. While exhibiting reduced efficacy against mouse CXCR6 with an IC50 of 18 μM, ML339 demonstrates no significant inhibition of CXCR5, CXCR4, or the apelin receptor (APJ), with IC50 values exceeding 79 μM. This compound shows promise for advancing research focused on prostate cancer. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CCR6 Antagonist
IDOR-1117-2520 is a potent and selective reversible antagonist targeting CCR6. It effectively inhibits CCL20-mediated calcium influx with an IC50 of 63 nM and blocks β-arrestin recruitment to human CCR6, showing an IC50 of 30 nM in recombinant cell models. As a substrate of P-glycoprotein/MDR1, IDOR-1117-2520 is a valuable tool for investigating autoimmune diseases and skin inflammation in research settings. -
CXCR Receptor Inhibitor
SCH-900875 is a selective inhibitor of the CXCR3 receptor, known for its oral bioavailability and ability to penetrate the blood-brain barrier. By binding to CXCR3, it effectively prevents the interaction of ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways, which reduces inflammatory cell migration. This compound holds potential for investigating various autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis, as well as inflammatory conditions like psoriasis and inflammatory bowel disease. -
Anti-inflammatory agent
Emorfazone is a non-steroidal anti-inflammatory drug that functions primarily through the inhibition of bradykinin-like substances and kininogen release. This compound exhibits notable anti-inflammatory and analgesic properties, making it a valuable tool for research on pain management and inflammatory conditions. Its oral activity further expands its application in pharmacological studies aimed at understanding inflammatory pathways. -
Non-steroidal Anti-inflammatory Agent
Zoliprofen is a non-steroidal anti-inflammatory agent that primarily acts by antagonizing bradykinin, leading to significant suppression of bradykinin-induced edema and pain responses. It also exhibits a moderate inhibitory effect on arachidonic acid-induced edema and pain, while additionally inhibiting PGE2 synthesis in bovine vesicular gland microsomes. This dual action makes Zoliprofen a valuable tool for research applications focused on pain management and inflammatory processes. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB1R/iNOS Antagonist
(Rac)-Zevaquenabant is a potent cannabinoid receptor type 1 (CB1R) and iNOS antagonist, exhibiting a Ki value of 5.7 nM for CB1R. This compound is primarily utilized in studies related to liver fibrosis, providing valuable insights into its pathophysiology and potential therapeutic interventions. Its selective inhibition of CB1R and iNOS pathways makes it a significant tool for investigating cannabinoid signaling and its implications in fibrotic diseases. -
CXCR7 Antagonist
CXCR7 antagonist-1 functions as a CXCR7 antagonist by inhibiting the binding of the SDF-1 (CXCL12) and I-TAC (CXCL11) chemokines to the CXCR7 receptor. This inhibition plays a critical role in suppressing tumor cell proliferation and tumor growth, thereby providing potential therapeutic applications in cancer treatment. Additionally, CXCR7 antagonist-1 may be beneficial in the study and management of various inflammatory diseases and other pathologies associated with the CXCR7 pathway. -
CXCR7 Antagonist
CXCR7 antagonist-1 hydrochloride functions as an antagonist to the CXCR7 receptor, effectively inhibiting the binding of the SDF-1 chemokine (CXCL12) and I-TAC (CXCL11). This compound demonstrates significant potential in research related to tumor cell proliferation and formation, as well as in inflammatory diseases and other pathologies associated with CXCR7 signaling. Its ability to modulate chemokine receptor activity makes it a valuable tool for exploring therapeutic strategies in cancer and inflammation. -
mPGES-1 Inhibitor
Zaloglanstat is a selective microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, demonstrating an IC50 of 5 nM for human mPGES-1 while sparing COX-1 and COX-2 with IC50 values greater than 10 μM. It effectively inhibits the conversion of prostaglandin PGH2 to prostaglandin PGE2, thereby mitigating inflammation-related overproduction of PGE2 and alleviating pain. In vitro studies show that Zaloglanstat reduces IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts. It is applicable in research exploring asthma, osteoarthritis, and neurodegenerative diseases, and exhibits effective inhibition of PGE2 release in whole blood from pig and dog models with IC50 values of 161 nM and 154 nM, respectively. -
Anti-inflammatory Agent
3-Hydroxyxanthone is a xanthone compound recognized for its anti-inflammatory properties. It effectively inhibits NADPH-catalyzed lipid peroxidation in human umbilical vein endothelial cells (HUVECs) and suppresses TNF-alpha-induced ICAM-1 expression. This compound is utilized in research focused on understanding inflammatory processes and vascular endothelial function. -
AMPK/Nrf2 Activator
Fortunellin is a flavonoid that acts as an AMPK/Nrf2 activator, derived from the fruits of Fortunella margarita (kumquat). It demonstrates minimal toxicity in murine models and effectively reduces inflammation and reactive oxygen species (ROS) generation in H9C2 cells induced by lipopolysaccharide (LPS). By enhancing the AMPK/Nrf2 pathway, Fortunellin protects against fructose-induced inflammation and oxidative stress, making it a valuable tool for research in diabetic cardiomyopathy.
