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P2X Receptor

" in MedChemExpress (MCE) Product Catalog:

70

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2

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4

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1

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N5025

    P2X Receptor Apoptosis Inflammation/Immunology Cancer
    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 .
    Bullatine A
  • HY-139627

    P2X Receptor Inflammation/Immunology
    P2X receptor-1 is a potential inhibitor of P2X receptor for the research of pain and inflammation.
    <em>P2X</em> <em>receptor</em>-1
  • HY-108667

    P2X Receptor Others
    TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats .
    TNP-ATP triethylammonium
  • HY-101077

    Iso-PPADS tetrasodium is a P2X-purinoceptor antagonist. Iso-PPADS tetrasodium inhibits P2X1 and P2X3 receptor with IC50s of 43 nM and 84 nM. Iso-PPADS tetrasodium is protective against ventilator-induced brain injury (VIBI) .
    Iso-PPADS tetrasodium
  • HY-134262

    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 .
    8-Bromo-ATP
  • HY-136254
    BzATP triethylammonium salt
    2 Publications Verification

    P2X Receptor Inflammation/Immunology Cancer
    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 .
    BzATP triethylammonium salt
  • HY-19978

    RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7) .
    RO-3
  • HY-148558

    P2X Receptor Neurological Disease
    P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats .
    <em>P2X</em>7 <em>receptor</em> antagonist-3
  • HY-150059

    P2X Receptor Neurological Disease Inflammation/Immunology
    P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC50 value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation .
    <em>P2X</em>7 <em>receptor</em> antagonist-2
  • HY-101044
    PPADS tetrasodium
    1 Publications Verification

    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/Ca 2+ exchanger in guinea pig airway smooth muscle .
    PPADS tetrasodium
  • HY-155194

    Others Inflammation/Immunology
    P2X7 receptor antagonist-4 (Compound 14a) is a P2X7R antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC50 in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice .
    <em>P2X</em>7 <em>receptor</em> antagonist-4
  • HY-101588

    MK-7264; AF-219

    P2X Receptor Inflammation/Immunology
    Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis .
    Gefapixant
  • HY-101588A

    MK-7264 citrate; AF-219 citrate

    P2X Receptor Inflammation/Immunology
    Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis .
    Gefapixant citrate
  • HY-131502

    P2X Receptor Inflammation/Immunology
    Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage .
    Taspine
  • HY-108673

    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) .
    Ro 0437626
  • HY-135976

    P2X Receptor Neurological Disease Inflammation/Immunology
    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 .
    P2X3 antagonist 34
  • HY-128402

    P2X Receptor Neurological Disease
    P2X3-IN-1 (example 7) is an inhibitor of P2X3 receptor. P2X3-IN-1 can be used for neurogenic diseases research .
    P2X3-IN-1
  • HY-18725

    P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease .
    P2X7-IN-2
  • HY-134440A

    P2X Receptor Inflammation/Immunology
    α,β-Methylene ATP, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .
    α,β-Methylene-ATP
  • HY-14483
    AF-353
    1 Publications Verification

    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 .
    AF-353
  • HY-18725A

    P2X Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    P2X7-IN-2 TFA (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 TFA inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 TFA can be used for the research of autoimmunity, inflammation and cardiovascular disease .
    P2X7-IN-2 TFA
  • HY-108652

    P2X Receptor 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 .
    α,β-Methylene-ATP trisodium
  • HY-134440

    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 .
    α,β-Methylene-ATP dilithium
  • HY-108676

    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 .
    NF023 hexasodium
  • HY-50697
    A-740003
    10+ Cited Publications

    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.
    A-740003
  • HY-137451

    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 .
    Sivopixant
  • HY-145466

    P2X Receptor Neurological Disease
    EVT-401 (P2X7 receptor antagonist-1) is a purinergic P2X7 receptor antagonist. EVT-401 has efficacy of combating neuroinflammation .
    EVT-401
  • HY-124300

    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 .
    JNJ-54166060
  • HY-15568
    A-317491
    4 Publications Verification

    P2X Receptor Neurological Disease Inflammation/Immunology
    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 .
    A-317491
  • HY-15568A
    A-317491 sodium salt hydrate
    4 Publications Verification

    P2X Receptor Neurological Disease Inflammation/Immunology
    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 .
    A-317491 sodium salt hydrate
  • HY-100483
    A-804598
    3 Publications Verification

    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 .
    A-804598
  • HY-15487

    PF-04905428

    P2X Receptor Neurological Disease
    CE-224535 is a selective P2X7 receptor antagonist.
    CE-224535
  • HY-13954
    A 839977
    1 Publications Verification

    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 .
    A 839977
  • HY-143576

    P2X Receptor Neurological Disease
    P2X3 antagonist 37 is a potent P2X3 receptor antagonist with an IC50 of 32.45 nM for hP2X3 (WO2021115225A1, example 68) .
    P2X3 antagonist 37
  • HY-101308

    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 .
    MRS2179 tetrasodium
  • HY-101308A

    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 .
    MRS2179 tetrasodium hydrate
  • HY-151546

    P2X Receptor Neurological Disease
    MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
    MRS4596
  • HY-D0976

    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 .
    NF279
  • HY-19888

    GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .
    GSK-1482160
  • HY-N1478

    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 .
    Gardenoside
  • HY-123205

    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 .
    Oxatomide
  • HY-16322

    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 .
    Minodronic acid
  • HY-15469

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
    GW791343 dihydrochloride
  • HY-15470

    P2X Receptor Neurological Disease
    GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
    GW791343 trihydrochloride
  • HY-15488A
    A 438079 hydrochloride
    5+ Cited Publications

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

    P2X Receptor Neurological Disease
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079
  • HY-108669
    AZ10606120 dihydrochloride
    1 Publications Verification

    P2X Receptor Neurological Disease Cancer
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth .
    AZ10606120 dihydrochloride
  • HY-112461A
    NF449 octasodium
    1 Publications Verification

    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 .
    NF449 octasodium
  • HY-117508

    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.
    JNJ-54175446
  • HY-16322S

    YM-529-d4

    Isotope-Labeled Compounds P2X Receptor Apoptosis Cancer
    Minodronic acid-d4 is deuterium labeled Minodronic acid. 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[1][2].
    Minodronic acid-d4

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