Catalog No.
Product Name
Application
Product Information
Citations
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CXCR Antagonist
VUF5834 is a non-peptide antagonist of the chemokine receptor CXCR3, exhibiting both non-competitive antagonistic and inverse agonistic activities. This compound effectively inhibits the effects of the chemokines CXCL10 and CXCL11 on human CXCR3. Notably, VUF5834 demonstrates a slightly lower affinity for rodent CXCR3 compared to primate CXCR3, making it a useful tool for investigating CXCR3-mediated pathways in various biological research applications. -
peptide
Polyphemusin II-Derived Peptide (T140) is a potent CXCR4 inhibitor that effectively blocks HIV-1 entry into host cells. Its mechanism involves disrupting the interaction between CXCR4 and the HIV-1 envelope glycoprotein, offering a targeted approach to HIV research. Additionally, T140 has been shown to inhibit the binding of the anti-CXCR4 monoclonal antibody (12G5) to its receptor, making it a valuable tool for studying CXCR4-related pathways and potential therapeutic interventions in viral infections. -
CXCR4 Inhibitor
CXCR4-IN-1 is a selective inhibitor of the CXCR4 chemokine receptor, with an IC50 of 20 nM. This compound exhibits potential biological activity in modulating cellular responses associated with cancer progression, HIV infection, diabetic retinopathy, and inflammatory conditions. CXCR4-IN-1 is suitable for use in research applications focused on these disease processes, providing valuable insights into therapeutic targeting of the CXCR4 signaling pathway. -
CXCR4 Modulator
CXCR4 modulator-1 is a selective modulator of the CXCR4 receptor, exhibiting a potent EC50 value of 100 nM. This compound plays a critical role in various biological processes, including inflammation, cancer progression, and HIV pathology. CXCR4 modulator-1 is suitable for research applications focusing on anti-inflammatory mechanisms, anticancer therapies, and HIV treatment studies. -
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. -
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. -
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. -
Dopamine Receptor Antagonist
(S)-SCH-23390 hydrochloride is a potent dopamine D1-like receptor antagonist, specifically targeting the D1 and D5 receptor subtypes with Ki values of 0.2 nM and 0.3 nM, respectively. This compound is widely utilized in neuropharmacology research to elucidate the role of dopamine signaling in various physiological and pathological processes. Its application in investigating dopaminergic dysfunction makes it valuable for studies related to neurological disorders and therapeutic interventions. -
D2/D3R Agonist
Quinpirole hydrochloride functions as a high-affinity agonist for the dopamine D2 and D3 receptors. This compound is primarily utilized in research applications focused on neuropharmacology and the exploration of dopaminergic signaling pathways. Quinpirole hydrochloride serves as an important tool for studying the effects of dopamine receptor activation in various in vitro and in vivo models. -
Dopamine Receptor Agonist
Pramipexole is a selective dopamine D2-type receptor agonist that effectively penetrates the blood-brain barrier. It exhibits high affinity with Kis of 2.2 nM for the D2-type receptor, 3.9 nM for D2, 0.5 nM for D3, and 1.3 nM for D4 receptors. This compound is utilized in research related to Parkinson's disease and restless legs syndrome, supporting studies aimed at understanding and treating these neurological disorders. -
D2 Receptor Antagonist
Eticlopride hydrochloride is a selective antagonist of the dopamine D2 receptor, demonstrating high binding affinity for D2, α1-adrenergic, α2-adrenergic, and various serotonin receptors. This compound has KIs of 0.09 nM for D2, 112 nM for α1, 699 nM for α2, 6220 nM for 5HT1, and 830 nM for 5HT2. Eticlopride hydrochloride is primarily utilized in research related to antipsychotic mechanisms and dopamine signaling pathways. -
D1/D5 Dopamine Receptor Agonist
Dihydrexidine hydrochloride is a potent and selective agonist of the D1-like dopamine receptors (D1/D5), exhibiting an IC50 of 10 nM for the D1 receptor. This compound demonstrates significant antiparkinsonian activity, making it valuable in neurological research. Additionally, Dihydrexidine hydrochloride has been shown to stimulate YAP phosphorylation, indicating its potential role in cellular signaling studies. -
Dopamine D2 Receptors Agonist
Lisuride is an orally active agonist of the dopamine D2 receptor, primarily utilized in neurological research. This ergot derivative is valuable for investigating conditions such as Parkinson's disease, migraine disorders, and hyperprolactinemia. Its ability to modulate dopamine activity makes Lisuride a significant compound for studying dopaminergic pathways and associated therapeutic strategies. -
Na+/Ca2+ Channel Blocker
Flunarizine is a potent dual blocker of Na+ and Ca2+ channels, specifically targeting T-type channels. It acts as a D2 dopamine receptor antagonist, exhibiting notable anticonvulsive and antimigraine properties. Additionally, flunarizine demonstrates peripheral vasodilatory effects, making it useful in research related to neurological disorders and vascular function. -
Antipsychotic Drug
Piperacetazine is a phenothiazine antipsychotic that primarily functions as a dopamine receptor antagonist. It has demonstrated inhibitory effects on the transcriptional activity of the PAX3::FOXO1 fusion protein, along with antitumor activity, exhibiting an IC50 of 7.627 μM against PANC-1 cells. This compound is applicable in research related to schizophrenia, pancreatic cancer, and other tumor types, making it a valuable tool for studying both neuropsychiatric disorders and cancer biology. -
Dopamine Receptor Antagonist
Tetrahydroberberine is a potent dopamine D2 receptor antagonist, which modulates dopaminergic signaling pathways. Its biological activity includes potential gastrointestinal benefits, such as enhancing gastric function and alleviating gastric pressure. This compound is of interest in research applications focused on neuropharmacology and gastrointestinal physiology. -
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. -
Dopamine D2 Receptor Agonist
MLS1547 is a potent G protein-biased agonist of the dopamine D2 receptor (D2R) with a Ki value of 1.2 μM. It effectively stimulates G protein-mediated signaling pathways, exhibiting an EC50 of 0.37 μM in calcium mobilization assays. Additionally, MLS1547 functions as an antagonist for dopamine-stimulated β-arrestin recruitment to the D2R, demonstrating an IC50 of 9.9 μM. This compound is valuable for investigating D2R signaling mechanisms and exploring therapeutic strategies for disorders associated with dopamine dysregulation. -
Dopamine Receptor Antagonist
Zuclopenthixol is a thioxanthene derivative that functions as a mixed antagonist of dopamine D1 and D2 receptors. This compound has demonstrated antipsychotic properties and is primarily utilized in research related to neuropharmacology and the treatment of schizophrenia. Its ability to modulate dopaminergic signaling makes it a valuable tool for studying dopamine-related disorders and therapeutic interventions.
