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-100483
    A-804598
    		Antagonist 98.68%
    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-19427A
    AZD9056 hydrochloride
    		Inhibitor 98.18%
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
    AZD9056 hydrochloride
  • 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-P0170
    TB500
    		Agonist 99.48%
    TB500 is a synthetic version of an active region of thymosin β4. TB500 exhibits anti-fibrotic and wound healing activities by inhibiting the Akt signaling pathway and binding to actin. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation.
    TB500
  • 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-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-19888
    GSK-1482160
    		Modulator 98.67%
    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-14483
    AF-353
    		Antagonist 99.53%
    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-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-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-101910
    PSB-12062
    		Antagonist 98.70%
    PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
    PSB-12062
  • HY-150270A
    NP-1815-PX sodium
    		Antagonist 99.62%
    NP-1815-PX sodium is a potent and selective P2X4R antagonist. NP-1815-PX sodium has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX sodium also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions.
    NP-1815-PX sodium
  • HY-109067A
    Opiranserin hydrochloride
    		Antagonist 99.62%
    Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin hydrochloride
  • 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-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-108675
    PPNDS tetrasodium
    		Antagonist
    PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers.
    PPNDS tetrasodium
  • HY-16322
    Minodronic acid
    		Antagonist 99.67%
    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-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-B1901
    Eperisone hydrochloride
    		Antagonist 99.95%
    Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex.
    Eperisone hydrochloride
  • HY-N5025
    Bullatine A
    		Inhibitor ≥98.0%
    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
P2X Receptor Isoform Comparison

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