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-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-170804
    P2X4 antagonist-3
    		Inhibitor
    P2X4 antagonist-3 (Compound 14c) is a P2X4 antagonist with an IC50 value of 1.2 μM. P2X4 antagonist-3 is promising for research of neuroinflammation, chronic pain, and cancer progression.
    P2X4 antagonist-3
  • HY-168474
    P2X4 antagonist-4
    		Antagonist
    P2X4 antagonist-4 (compound 64) is a potent P2X4R antagonist with an IC50 value of 8 µM. P2X4 antagonist-4 blocks the ATP-induced NLRP3 inflammasome activation and release of IL-1β.
    P2X4 antagonist-4
  • 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 (YM-529-d4) is deuterium labeled Minodronic acid (HY-16322). Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.
    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
  • HY-143890
    MRS4738
    		Antagonist
    MRS4738 is a potent and high affinity P2Y14R antagonist. MRS4738 exhibits anti-hyperallodynic and antiasthmatic activity in vivo.
    MRS4738
  • 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-178230
    EVT‑401
    		Agonist
    EVT‑401 is an anti-inflammatory agent. EVT‑401 can be metabolized and exert pharmacological effects in vivo. EVT‑401 can be used for research on inflammatory conditions.
    EVT‑401
  • HY-161914
    P2X3 antagonist 39
    		Antagonist
    P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model.
    P2X3 antagonist 39
  • HY-137610A
    TNP-ATP tetrasodium
    		Antagonist
    TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors (IC50 = 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors). TNP-ATP reduces acetate-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively). TNP-ATP dose-dependently attenuates acetate-induced abdominal contractions in a mouse visceral pain model (ED50 = 6.35 µmol/kg)[1][2].
    TNP-ATP tetrasodium
  • HY-176731
    MSK-9
    		Modulator
    MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).
    MSK-9
  • HY-124300
    JNJ-54166060
    		Antagonist
    JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.
    JNJ-54166060
  • HY-160677
    P2X4 antagonist-2
    		Antagonist
    P2X4 antagonist-2 is an antagonist for P2X4 with an IC50 of 24 nM.
    P2X4 antagonist-2
  • HY-183784
    P2X7R antagonist-1
    		Antagonist
    P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research.
    P2X7R antagonist-1
  • HY-134458A
    H-Lys-Tyr-OH TFA
    H-Lys-Tyr-OH TFA (Lysyltyrosine TFA) is a dipeptide composed of lysine and tyrosine. H-Lys-Tyr-OH TFA prevents neurological diseases or improves brain function by promoting the release of noradrenaline and tyrosine into the brain.
    H-Lys-Tyr-OH TFA
  • HY-151547
    MRS4719
    		Antagonist
    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
  • HY-151546S
    MRS4596-d4
    MRS4596-d4 is the deuterium labeled MRS4596 (HY-151546). 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-d<sub>4</sub>
P2X Receptor Isoform Comparison

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