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-109173
    Filapixant
    		Antagonist 98.78%
    Filapixant is a purinoreceptor antagonist extracted from patent WO2016091776A1, example 348. Filapixant is the active reference substance of Eliapixant.
    Filapixant
  • 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-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-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-19978
    RO-3
    		Antagonist
    RO-3 is a potent, CNS-penetrant, 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-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-16322A
    Minodronic acid hydrate
    		Antagonist 99.67%
    Minodronic acid (YM-529) hydrate 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 hydrate
  • HY-131502
    Taspine
    		Inhibitor
    Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage.
    Taspine
  • 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-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-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-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
  • HY-153710
    P2X3 antagonist 38
    		Antagonist
    P2X3 antagonist 38 (compound 4) is a potent and orally active P2X3 antagonist with IC50 values of 0.132, 0.165, 0.421 µM for hP2X3, rP2X3, gpP2X3, respectively.
    P2X3 antagonist 38
  • HY-P1330
    Purotoxin 1
    		Inhibitor
    Purotoxin 1 is a P2X3 receptor inhibitor. Purotoxin 1 shows antinociceptive properties in animal models of inflammatory pain. Purotoxin 1 can be isolated from the venom of the wolf spider Geolycosa sp.
    Purotoxin 1
  • HY-16322S
    Minodronic acid-d4
    		Antagonist
    Minodronic acid-d4 is deuterium labeled Minodronic acid. 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[1][2].
    Minodronic acid-d<sub>4</sub>
  • HY-124300A
    (S)-JNJ-54166060
    (S)-JNJ-54166060 is an enantiomer of JNJ 54166060. JNJ 54166060 is a potent P2X7 antagonist.
    (S)-JNJ-54166060
  • HY-130284
    NF864
    		Inhibitor
    NF864 is a selectivelyP2X1 receptorinhibitor in human platelets.
    NF864
  • HY-151546
    MRS4596
    		Antagonist
    MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
    MRS4596
P2X Receptor Isoform Comparison

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