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-145466
    EVT-401
    		Inhibitor 99.78%
    EVT-401 is an orally active, potent and highly selective P2X7R inhibitor, with an IC50 of 10 nM and a Ki of 7.6 nM for human P2X7R, and an IC50 of 220 nM for mouse P2X7R. EVT-401 promots apoptosis and inducs cell cycle arrest in RA SF, reducs the production of proinflammatory and joint-destructive mediators, and mitigats aggressive phenotypes. EVT-401 exhibits favorable oral bioavailability and a good safety profile, making it suitable for research into rheumatoid arthritis.
    EVT-401
  • HY-123481
    JNJ-42253432
    		Antagonist 98.15%
    JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
    JNJ-42253432
  • HY-108670
    AZ 11645373
    		Antagonist 99.54%
    AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM.
    AZ 11645373
  • HY-15469
    GW791343 dihydrochloride
    		Inhibitor 98.53%
    GW791343 dihydrochloride 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 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
    GW791343 dihydrochloride
  • HY-137451A
    (E/Z)-Sivopixant
    		Antagonist 98.64%
    (E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.
    (E/Z)-Sivopixant
  • HY-109173
    Filapixant
    		Antagonist 98.78%
    Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough.
    Filapixant
  • 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.
    P2X3-IN-1
  • HY-19978
    RO-3
    		Antagonist
    RO-3 is a potent, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7).
    RO-3
  • HY-18745
    BzATP triethylammonium
    		Agonist
    BzATP triethylammonium 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 is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.
    BzATP triethylammonium
  • HY-160645
    P2X4 antagonist-1
    		Antagonist 99.89%
    P2X4 antagonist-1 is a P2X4 receptor antagonist with an IC50 of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer.
    P2X4 antagonist-1
  • HY-108673
    Ro 0437626
    		Antagonist
    Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM).
    Ro 0437626
  • HY-108671
    NF110
    		Antagonist
    NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons.
    NF110
  • HY-101370
    2-Methylthio-ATP tetrasodium
    		Activator 98.0%
    2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation.
    2-Methylthio-ATP tetrasodium
  • HY-124857
    7DG
    		Inhibitor 98%
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders.
    7DG
  • HY-18725A
    P2X7-IN-2 TFA
    		Inhibitor 99.93%
    P2X7-IN-2 TFA (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 TFA inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 TFA can be used for the research of autoimmunity, inflammation and cardiovascular disease.
    P2X7-IN-2 TFA
  • HY-B1901R
    Eperisone hydrochloride (Standard)
    		Antagonist
    Eperisone (hydrochloride) (Standard) is the analytical standard of Eperisone (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-18725
    P2X7-IN-2
    		Inhibitor
    P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease.
    P2X7-IN-2
  • HY-151547S
    MRS4719-d3
    MRS4719-d3 is the deuterium labeled MRS4719 (HY-151547). MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
    MRS4719-d<sub>3</sub>
  • HY-D1199
    Blue FPG-A trisodium
    		Antagonist
    Blue FPG-A trisodium is a selective antagonist of P2X1 receptor and P2Y1 receptor with IC50 values of 35.5 μM and 2.6 μM, respectively. Blue FPG-A trisodium is a structural isomer of the components of Reactive Blue 2 (RB2).
    Blue FPG-A trisodium
  • HY-14483A
    AF-353 hydrochloride
    		Antagonist
    AF-353 hydrochloride 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 hydrochloride
P2X Receptor Isoform Comparison

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