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-108960
    PPADS
    Antagonist
    PPADS is a P2 receptor antagonist, with IC50s of 68 nM (P2X1) and 214 nM (P2X3). PPADS acts as an ATP (nucleotide) mimetic and competes with ATP for its binding site on P2 receptors. PPADS is also a reversible competitive antagonist of the NAADP receptor. PPADS reverses nociceptive hypersensitivity and reduces the increased NO/NOS system and IL-1β in both peripheral and central steps of nervous system.
    PPADS
  • HY-134440
    α,β-Methylene-ATP dilithium
    Agonist
    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-19427
    AZD9056
    Antagonist
    AZD9056 is a P2X7 purinergic receptor antagonist with anticancer activity. AZD9056 can inhibit the invasion and metastasis of cancer stem cells.
    AZD9056
  • HY-134370
    Ap4G
    Ap4G is a dinucleoside polyphosphate compound with vasoconstrictor activity. Ap4G regulates vasoconstriction through P2 receptors, especially P2X receptors, and is an important tool for studying vascular physiology and pathology.
    Ap4G
  • HY-129731
    Lappaconine
    Inhibitor
    Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters.
    Lappaconine
  • HY-122272S
    Paroxetine-d4
    Inhibitor
    Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>4</sub>
  • HY-15470
    GW791343 trihydrochloride
    Inhibitor
    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-156986
    ITH15004
    Antagonist
    ITH15004 is a CNS-penetrated P2X7 antagonist, used for the study of neurodegenerative diseases.
    ITH15004
  • HY-137606
    Uridine adenosine tetraphosphate
    Uridine adenosine tetraphosphate (UP4A) is an endothelium-derived vasoconstrictor that primarily acts through the P2X1 receptor and possibly through the P2Y2 and P2Y4 receptors. Uridine adenosine tetraphosphate can be used in the study of cardiovascular diseases.
    Uridine adenosine tetraphosphate
  • HY-101588R
    Gefapixant (Standard)
    Antagonist
    Gefapixant (Standard) is the analytical standard of Gefapixant. This product is intended for research and analytical applications. 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 (Standard)
  • HY-112461
    NF449
    Antagonist
    NF449 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 is a G-selective G Protein antagonist. NF449 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
  • HY-W097612
    P2X4 antagonist-5
    Control
    P2X4 antagonist-5 (compound 63) is a control compound for P2X4 antagonists (IC50>100 μM, hP2X4).
    P2X4 antagonist-5
  • HY-123205R
    Oxatomide (Standard)
    Antagonist
    Oxatomide (Standard) is the analytical standard of Oxatomide. This product is intended for research and analytical applications. 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 Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
    Oxatomide (Standard)
  • HY-108668
    TC-P 262
    Inhibitor
    TC-P 262 is a potent P2X3 inhibitor. TC-P 262 shows inhibition by bindings to hP2X3. TC-P 262 has the potential for the research of rheumatoid arthritis, cough, and pain.
    TC-P 262

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