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CX3C chemokine receptor1

" in MedChemExpress (MCE) Product Catalog:

842

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2

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3

Fluorescent Dye

7

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141

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18

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82

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402

Recombinant Proteins

51

Isotope-Labeled Compounds

54

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7

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2518

    Protease Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
    Protease-Activated Receptor-1, PAR-1 Agonist
  • HY-P2518A

    Protease Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
    Protease-Activated Receptor-1, PAR-1 Agonist TFA
  • HY-10634
    AMG 517
    5+ Cited Publications

    TRP Channel Neurological Disease
    AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
    AMG 517
  • HY-164817

    Cannabinoid Receptor Cancer
    CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research [1].
    CB1/2 receptor-1
  • HY-143313

    Protease Activated Receptor (PAR) Cardiovascular Disease
    Protease-Activated Receptor-1 antagonist 1 (Compound 13) is a protease-activated receptor-1 (PAR-1) antagonist with the IC50 of 3 nM by FLIPR technology. Protease-Activated Receptor-1 antagonist 1 can be used for the research of thrombotic cardiovascular, myocardial infarction, and peripheral arterial disease [1].
    Protease-Activated Receptor-1 antagonist 1
  • HY-143315

    Protease Activated Receptor (PAR) Cardiovascular Disease
    Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K + channel with an IC50 value of 9 µM [1].
    Protease-Activated Receptor-1 antagonist 3
  • HY-143314

    Protease Activated Receptor (PAR) Cardiovascular Disease
    Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis [1].
    Protease-Activated Receptor-1 antagonist 2
  • HY-139627

    P2X Receptor Inflammation/Immunology
    P2X receptor-1 is a potential inhibitor of P2X receptor for the research of pain and inflammation.
    P2X receptor-1
  • HY-18076

    LPL Receptor Infection Inflammation/Immunology
    LPA1 receptor antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.
    LPA1 receptor antagonist 1
  • HY-13338S

    Isotope-Labeled Compounds Adrenergic Receptor Cardiovascular Disease Inflammation/Immunology
    Mabuterol-d9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor[1].
    Mabuterol-d9
  • HY-P9903
    Nivolumab
    15+ Cited Publications

    BMS-936558; ONO-4538; MDX-1106

    PD-1/PD-L1 Cancer
    Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.
    Nivolumab
  • HY-136152

    MCHR1 (GPR24) Metabolic Disease Endocrinology
    MCHR1 antagonist 3 is a potent the melanin-concentrating hormone receptor-1 (MCHR1) antagonist. MCHR1 antagonist 3 is used to regulate energy metabolism [1].
    MCHR1 antagonist 3
  • HY-138097
    α-NETA
    5+ Cited Publications

    Chemerin Receptor Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis Cancer
    α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity [1] .
    α-NETA
  • HY-18200

    E5555; ER-172594-00

    Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease [1] .
    Atopaxar
  • HY-18200B

    E5555 hydrobromide; ER 172594-06

    Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease [1] .
    Atopaxar hydrobromide
  • HY-B0190

    Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease Infection Cancer
    Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall [1] [3] .
    Nafamostat
  • HY-B0190B

    Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease Infection Cancer
    Nafamostat hydrochloride, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat hydrochloride has anticancer and antivirus effect. Nafamostat hydrochloride induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat hydrochloride can be used in the development of the pathological thickening of the arterial wall [1] [3] .
    Nafamostat hydrochloride
  • HY-P99218

    Sch 717454; 19D12

    IGF-1R Cancer
    Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research [1] .
    Robatumumab
  • HY-B0190A
    Nafamostat mesylate
    10+ Cited Publications

    FUT-175

    Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease Infection Cancer
    Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall [1] [3] .
    Nafamostat mesylate
  • HY-N1881

    Lipoxygenase Glycosidase Others
    4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
    4',5-Dihydroxyflavone
  • HY-P99203

    PD-1/PD-L1 Cancer
    Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research [1] .
    Cemiplimab
  • HY-15103

    PTHR Androgen Receptor Cancer
    AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) [1] .
    AH3960
  • HY-143312D

    GLP Receptor Metabolic Disease
    (R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R [1].
    (R)-V-0219 hydrochloride
  • HY-115832

    Others Cancer
    Ap44mSe is a selenosemicarbazone that effectively depletes cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regulated gene-1. Ap44mSe forms redox active Cu complexes that target the lysosome to induce lysosomal membrane permeabilization [1].
    Ap44mSe
  • HY-143312B

    GLP Receptor Metabolic Disease
    (R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R [1].
    (R)-V-0219
  • HY-113008AS

    (Z)-Urocanic acid-13C3; cis-UCA-13C3

    Isotope-Labeled Compounds 5-HT Receptor Inflammation/Immunology
    cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
    cis-Urocanic acid-13C3
  • HY-107146

    P1pal-7

    Protease Activated Receptor (PAR) Cardiovascular Disease Cancer
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects [1] [3] .
    PZ-128
  • HY-115831

    S1P1 agonist 3

    LPL Receptor Cardiovascular Disease
    SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome [1] [3] .
    SAR247799
  • HY-143312C

    GLP Receptor Metabolic Disease
    (S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice [1].
    (S)-V-0219
  • HY-143312E

    GLP Receptor Metabolic Disease
    (S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice [1].
    (S)-V-0219 hydrochloride
  • HY-16734A

    MT-1303 hydrochloride

    LPL Receptor Cancer
    Amiselimod hydrochloride is an orally active novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod-P shows potent and high selectivity for S1P1 and S1P5 but with minimal agonist activity for S1P4 and no distinct agonist activity for S1P2 or S1P3. Amiselimod hydrochloride is promising for research of autoimmune diseases [1] .
    Amiselimod hydrochloride
  • HY-103360A

    UCB35625

    CCR Inflammation/Immunology
    cis-J-113863 is a competitive chemokine receptor 1 (CCR1) antagonist, with IC50 values of 0.9 and 5.8 nM for human and mouse CCR1 receptors, respectively [1].
    cis-J-113863
  • HY-103286

    Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
    PD176252
  • HY-18200A

    E5555 hydrochloride; ER-172594-00 hydrochloride

    Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease [1] [3].
    Atopaxar hydrochloride
  • HY-P1345A
    TLQP-21 TFA
    1 Publications Verification

    Complement System Neurological Disease Endocrinology
    TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions [1] .
    TLQP-21 TFA
  • HY-14977

    LPL Receptor Inflammation/Immunology
    CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) [1].
    CS-0777-P
  • HY-147385

    CCR Inflammation/Immunology
    CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [ 125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM) [1].
    CCR4 antagonist 3
  • HY-P10300

    IL-8 (54-72)

    CXCR Inflammation/Immunology
    CXCL8 (54-72) is a C-terminal peptide based on the chemokine CXCL8. CXCL8 (54-72) has an interaction between a long and highly positively charged C-terminal region and a negative charge on the GAG that binds to the GAG. CXCL8 (54-72) can inhibit the adhesion and migration of neutrophils and adhesion of endothelial cells. CXCL8 (54-72) can be used to study chemokines in inflammatory response [1].
    CXCL8 (54-72)
  • HY-D2201

    Fluorescent Dye Cancer
    Fluorescent ACKR3 antagonist 1(compound 18a) is a atypical chemokine receptor 3 antagonist [1].
    Fluorescent ACKR3 antagonist 1
  • HY-123813

    Arrestin Cancer
    CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) [1].
    CCX-777
  • HY-139643

    CXCR Inflammation/Immunology Cancer
    CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128) [1].
    CXCR7 antagonist-1
  • HY-139643A

    CXCR Inflammation/Immunology Cancer
    CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128) [1].
    CXCR7 antagonist-1 hydrochloride
  • HY-15545

    CCR Neurological Disease Inflammation/Immunology Endocrinology
    AZD-4818 is a potent antagonist of chemokine CCR1. AZD-4818 can be used for researching chronic obstructive pulmonary disease (COPD) [1].
    AZD-4818
  • HY-116835

    CCR Inflammation/Immunology
    BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research [1].
    BI-6901
  • HY-135891

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux [1] [3].
    AZD2423
  • HY-145640

    AZD4721; RIST4721

    CXCR Inflammation/Immunology
    Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease [1].
    Vimnerixin
  • HY-15319
    AMG 487
    20+ Cited Publications

    CXCR Inflammation/Immunology Endocrinology Cancer
    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively [1].
    AMG 487
  • HY-15252
    Reparixin L-lysine salt
    Maximum Cited Publications
    52 Publications Verification

    Repertaxin L-lysine salt

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
    Reparixin L-lysine salt
  • HY-163761

    CCR Others
    LT166 is a fluorescent ligand for CC chemokine receptor 1 (CCR1) with a KD of 1.90 μM [1].
    LT166
  • HY-15319A

    CXCR Cancer
    (±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively [1].
    (±)-AMG 487

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