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Targets Recommended: P2X Receptor
Results for "

P2X Receptor

" in MCE Product Catalog:

41

Inhibitors & Agonists

4

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-136254
    BzATP triethylammonium salt

    P2X Receptor Cancer Inflammation/Immunology
    BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively. BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.
  • HY-108673
    Ro 0437626

    P2X Receptor Cancer
    Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM).
  • HY-134262
    8-Bromo-ATP

    8-Bromoadenosine 5'-triphosphate; 8-Br-ATP

    P2X Receptor Cancer
    8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM.
  • HY-135976
    P2X3 antagonist 34

    P2X Receptor Inflammation/Immunology Neurological Disease
    P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
  • HY-N5025
    Bullatine A

    P2X Receptor Apoptosis Cancer Inflammation/Immunology
    Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
  • HY-14483
    AF-353

    Ro-4

    P2X Receptor Cancer
    AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
  • HY-108652
    α,β-Methylene ATP trisodium

    Others Inflammation/Immunology
    α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP trisodium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
  • HY-134440
    α,β-Methylene-ATP dilithium

    P2X Receptor Inflammation/Immunology
    α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
  • HY-108676
    NF023 hexasodium

    P2X Receptor Neurological Disease
    NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively.
  • HY-137451
    Sivopixant

    S-600918

    P2X Receptor Neurological Disease
    Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-50697
    A-740003

    P2X Receptor Neurological Disease
    A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
  • HY-15568A
    A-317491 sodium salt hydrate

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • HY-15568
    A-317491

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • HY-124300
    JNJ-54166060

    P2X Receptor Others
    JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.
  • HY-D0976
    NF279

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env.
  • HY-100483
    A-804598

    P2X Receptor Cancer
    A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
  • HY-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-15487
    CE-224535

    PF-04905428

    P2X Receptor Neurological Disease
    CE-224535 is a selective P2X7 receptor antagonist.
  • HY-101308
    MRS2179 tetrasodium

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
  • HY-101308A
    MRS2179 tetrasodium hydrate

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.
  • HY-101588
    Gefapixant

    MK-7264; AF-219

    P2X Receptor Inflammation/Immunology
    Gefapixant (MK-7264) is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
  • HY-N1478
    Gardenoside

    Others Neurological Disease
    Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
  • HY-16322
    Minodronic acid

    YM-529

    P2X Receptor Apoptosis Cancer
    Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.
  • HY-108669
    AZ10606120 dihydrochloride

    P2X Receptor Cancer Neurological Disease
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-15488
    A 438079

    P2X Receptor Neurological Disease
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-15488A
    A 438079 hydrochloride

    P2X Receptor Neurological Disease
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-123205
    Oxatomide

    Histamine Receptor P2X Receptor 5-HT Receptor Inflammation/Immunology
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
  • HY-109170
    Eliapixant

    BAY 1817080

    P2X Receptor Inflammation/Immunology
    Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.
  • HY-137451A
    (E/Z)-Sivopixant

    (E/Z)-S-600918

    P2X Receptor Inflammation/Immunology
    (E/Z)-Sivopixant (Compound I-127) is a potent P2X3 receptor antagonist with an IC50 of 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.
  • HY-117508
    JNJ-54175446

    P2X Receptor Neurological Disease
    JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
  • HY-134807
    Indophagolin

    P2X Receptor 5-HT Receptor Autophagy Cancer
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
  • HY-N7740
    Adenosine 2',5'-diphosphate sodium

    P2Y Receptor Endogenous Metabolite Others
    Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors.
  • HY-110237
    BX430

    P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
  • HY-108671
    NF110

    P2X Receptor Neurological Disease
    NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons.
  • HY-13290
    KN-62

    CaMK P2X Receptor Autophagy Metabolic Disease Cancer
    KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-101911
    5-BDBD

    P2X Receptor Neurological Disease
    5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.