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 (87):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    BzATP triethylammonium salt
  • 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.
    A-740003
  • HY-103259
    Sodium metatungstate
    Sodium metatungstate (Sodium polyoxotungstate) is a NTPDase inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively. Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission.
    Sodium metatungstate
  • 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.
    KN-62
  • HY-15488A
    A 438079 hydrochloride
    Antagonist 99.92%
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 hydrochloride
  • HY-130284
    NF864
    Inhibitor
    NF864 is a selectivelyP2X1 receptorinhibitor in human platelets.
    NF864
  • HY-101077
    Iso-PPADS tetrasodium
    Antagonist
    Iso-PPADS tetrasodium is a P2X-purinoceptor antagonist. Iso-PPADS tetrasodium inhibits P2X1 and P2X3 receptor with IC50s of 43 nM and 84 nM. Iso-PPADS tetrasodium is protective against ventilator-induced brain injury (VIBI).
    Iso-PPADS tetrasodium
  • HY-156986
    ITH15004
    Antagonist
    ITH15004 is a CNS-penetrated P2X7 antagonist, used for the study of neurodegenerative diseases.
    ITH15004
  • 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.
    NF449 octasodium
  • 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.
    Aurintricarboxylic acid
  • 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.
    Gefapixant
  • 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.
    JNJ-47965567
  • HY-101044
    PPADS tetrasodium
    Antagonist
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle.
    PPADS tetrasodium
  • HY-15488
    A 438079
    Antagonist 99.74%
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079
  • 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.
    α,β-Methylene-ATP trisodium
  • 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.
    JNJ-55308942
  • 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.
    BAY-1797
  • 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.
    AZD9056 hydrochloride
  • 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).
    5-BDBD
  • 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 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