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.

P2X Receptor Related Products (85):

Cat. No. Product Name Effect Purity
  • HY-136254
    BzATP triethylammonium salt
    Agonist
    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.
  • HY-50697
    A-740003
    Antagonist 99.20%
    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.
  • HY-13290
    KN-62
    Antagonist 99.45%
    KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-15488A
    A 438079 hydrochloride
    Antagonist 99.92%
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-122575
    Aurintricarboxylic acid
    Antagonist
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
  • HY-128402
    P2X3-IN-1
    Inhibitor
    P2X3-IN-1 (example 7) is an inhibitor of P2X3 receptor. P2X3-IN-1 can be used for neurogenic diseases research.
  • HY-137888A
    Oxidized ATP trisodium salt
    Inhibitor
    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.
  • HY-150270A
    NP-1815-PX sodium
    Antagonist
    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.
  • HY-101588
    Gefapixant
    Antagonist 99.32%
    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.
  • HY-112461A
    NF449 octasodium
    Antagonist ≥99.0%
    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.
  • HY-101418
    JNJ-47965567
    Antagonist 99.77%
    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.
  • HY-123857
    JNJ-55308942
    Antagonist 99.95%
    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.
  • HY-19427A
    AZD9056 hydrochloride
    Inhibitor 98.82%
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
  • HY-108652
    α,β-Methylene-ATP trisodium
    Agonist 99.75%
    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.
  • HY-130605
    BAY-1797
    Antagonist 99.42%
    BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects.
  • HY-101911
    5-BDBD
    Antagonist 99.79%
    5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
  • HY-15488
    A 438079
    Antagonist 99.74%
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-108669
    AZ10606120 dihydrochloride
    Antagonist 99.38%
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-135976
    P2X3 antagonist 34
    Antagonist 99.71%
    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.
  • HY-117508
    JNJ-54175446
    Antagonist 99.49%
    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.