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

P2X Receptor

P2XRs

P2X Receptor

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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.

P2X Receptor Isoform Specific Products:

P2X Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101418
    JNJ-47965567
    		Antagonist 99.79%
    JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
    JNJ-47965567
  • HY-113273A
    Diadenosine pentaphosphate pentasodium
    		Inhibitor 99.13%
    Diadenosine pentaphosphate pentasodium is an agonist and negative modulator of the P2X1 receptor, an endogenous vasoactive purine dinucleotide that can be isolated from platelets. Diadenosine pentaphosphate pentasodium mediates negative regulation of dendrite growth and number by activating homologous and heterologous P2X1 receptors, which triggers a transient and moderate increase in intracellular calcium levels within dendritic growth cones. Diadenosine pentaphosphate pentasodium is widely present in secretory vesicles such as platelets, chromaffin cells and brain synaptosomes, and exhibits selective activity on dendrite growth of cultured hippocampal neurons, inhibiting only dendrite growth without affecting axon growth. Diadenosine pentaphosphate pentasodium has a weaker ability to compete with RcCHAD for binding to polyP than short-chain polyPs.
    Diadenosine pentaphosphate pentasodium
  • HY-108669
    AZ10606120 dihydrochloride
    		Antagonist 99.93%
    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-100483
    A-804598
    		Antagonist 98.68%
    A-804598 is a BBB 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-15568
    A-317491
    		Antagonist 98.64%
    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-110237
    BX430
    		Antagonist 99.21%
    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.
    BX430
  • HY-W033577
    Tricarbonyldichlororuthenium(II) dimer
    		Antagonist 98.0%
    Tricarbonyldichlororuthenium(II) dimer (CORM-2) is a CO-releasing molecule. Tricarbonyldichlororuthenium(II) dimer exhibits anti-inflammatory, antioxidant, and gastric mucosa-protective activities. Additionally, Tricarbonyldichlororuthenium(II) dimer has CO-independent functional effects on multiple potassium channels.
    Tricarbonyldichlororuthenium(II) dimer
  • HY-123205
    Oxatomide
    		Antagonist 98.11%
    Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.
    Oxatomide
  • HY-14483
    AF-353
    		Antagonist 99.43%
    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-164426
    HEI3090
    		Activator 99.00%
    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-150270A
    NP-1815-PX sodium
    		Antagonist 99.51%
    NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis).
    NP-1815-PX sodium
  • HY-19888
    GSK-1482160
    		Modulator 98.67%
    GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
    GSK-1482160
  • HY-123857
    JNJ-55308942
    		Antagonist 99.92%
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
    JNJ-55308942
  • HY-137888A
    Oxidized ATP trisodium salt
    		Inhibitor 98.0%
    Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis.
    Oxidized ATP trisodium salt
  • HY-108676
    NF023 hexasodium
    		Antagonist 99.99%
    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-108667
    TNP-ATP triethylammonium
    		Antagonist 98.70%
    TNP-ATP triethylammonium is a P2X receptor antagonist with an IC50 of 0.010 μM for P2X3 and an IC50 of 0.062 μM for P2X2/3. TNP-ATP triethylammonium acts as an inhibitor of CheA autophosphorylation, with a Ki of 0.7 µM. TNP-ATP triethylammonium blocks the functional activation of P2X1-7 receptors. TNP-ATP triethylammonium attenuates hypoxia-induced IL-1β expression and release. TNP-ATP triethylammonium alleviates visceral pain, and improves hypoxia-induced cognitive impairment, insufficient myelination and neuroinflammation. Binding of TNP-ATP triethylammonium to CheA enhances the fluorescence of the TNP group. TNP-ATP triethylammonium can be used in studies related to visceral pain. NP-ATP triethylammonium can be used in studies related to hypoxia-induced insufficient myelination and cognitive decline.
    TNP-ATP triethylammonium
  • HY-101910
    PSB-12062
    		Antagonist 98.05%
    PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
    PSB-12062
  • HY-16322
    Minodronic acid
    		Antagonist 99.67%
    Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.
    Minodronic acid
  • 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-D0976
    NF279
    		Antagonist 98.5%
    NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC50 value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection.
    NF279
P2X Receptor Isoform Comparison

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