1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. P2X Receptor

P2X Receptor

P2XRs

P2X receptors are a family of seven (P2X1R-P2X7R) cation permeable ligand-gated ion channels (LGICs) that open in response to binding by the extracellular ligand, adenosine 5′-triphosphate (ATP). P2X receptors have a high permeability to Ca2+, Na+, and K+ and are expressed widely throughout the nervous, immune, cardiovascular, skeletal, gastrointestinal, respiratory, and endocrine systems.

P2X receptors are widely expressed in excitatory and non-excitatory cells, such as neuron, glia, platelet, epithelia and macrophage, and participate in many important physiological and pathological processes, including synaptic transmission, pain perception, inflammation, cardiovascular modulation, immunomodulation and tumorigenesis.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15568A
    A-317491 sodium salt hydrate
    Antagonist 99.88%
    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-117508
    JNJ-54175446
    Antagonist 99.30%
    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-109170
    Eliapixant
    Antagonist 99.95%
    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.
    Eliapixant
  • HY-N1478
    Gardenoside
    99.55%
    Gardenoside is an orally active natural compound found in Gardenia fruits. Gardenoside reliefs chronic constriction injury (CCI)-induced neuropathic pain by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside reduces reactive oxygen species (ROS). Gardenoside can be used for anti-inflammatory, antinociceptive and hepatoprotective study.
    Gardenoside
  • HY-108667
    TNP-ATP triethylammonium
    Antagonist 98.70%
    TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats.
    TNP-ATP triethylammonium
  • HY-132981
    Lu AF27139
    Antagonist 99.71%
    Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
    Lu AF27139
  • HY-15487
    CE-224535
    Antagonist 98.91%
    CE-224535 is a selective P2X7 receptor antagonist.
    CE-224535
  • HY-D0976
    NF279
    Antagonist ≥98.0%
    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-N9182
    Zeaxanthin dipalmitate
    ≥98.0%
    Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).
    Zeaxanthin dipalmitate
  • HY-15469
    GW791343 dihydrochloride
    Inhibitor 98.03%
    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-137451
    Sivopixant
    Antagonist 99.90%
    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-134807
    Indophagolin
    Antagonist 98.05%
    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.
    Indophagolin
  • HY-164426
    HEI3090
    Activator 99.04%
    HEI3090 is a P2X7R activator. HEI3090 stimulates dendritic cells expressing P2X7R to produce IL-18, which subsequently promotes Natural Killer cells and CD4 T cells within tumors to produce IFN-γ, leading to a sustained antitumor response. HEI3090 can be used to enhance the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC).
    HEI3090
  • HY-145466
    EVT-401
    Antagonist 99.89%
    EVT-401 (P2X7 receptor antagonist-1) is a purinergic P2X7 receptor antagonist. EVT-401 has efficacy of combating neuroinflammation.
    EVT-401
  • HY-150059
    P2X7 receptor antagonist-2
    Antagonist 99.21%
    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.
    P2X7 receptor antagonist-2
  • HY-105285
    Piromelatine
    Inhibitor 99.54%
    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.
    Piromelatine
  • HY-108671
    NF110
    Antagonist
    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.
    NF110
  • HY-101370
    2-Methylthio-ATP tetrasodium
    Activator ≥98.0%
    2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation.
    2-Methylthio-ATP tetrasodium
  • HY-101588A
    Gefapixant citrate
    Antagonist 99.23%
    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-109173
    Filapixant
    Antagonist 98.78%
    Filapixant is a purinoreceptor antagonist extracted from patent WO2016091776A1, example 348. Filapixant is the active reference substance of Eliapixant.
    Filapixant

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