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-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-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-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-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-160645
    P2X4 antagonist-1
    		Antagonist 99.89%
    P2X4 antagonist-1 (Compound 24) is an antagonist for P2X4 with IC50 of 15 nM.
    P2X4 antagonist-1
  • HY-143576
    P2X3 antagonist 37
    		Antagonist
    P2X3 antagonist 37 is a potent P2X3 receptor antagonist with an IC50 of 32.45 nM for hP2X3 (WO2021115225A1, example 68).
    P2X3 antagonist 37
  • HY-14485
    Ro-51
    		Antagonist
    Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain.
    Ro-51
  • HY-143568
    P2X3 antagonist 36
    		Antagonist
    P2X3 antagonist 36 is a P2X3 antagonist extracted from patent WO2019081343A1 compound 156.
    P2X3 antagonist 36
  • HY-134262
    8-Bromo-ATP
    		Agonist
    8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM.
    8-Bromo-ATP
  • HY-162951
    P2X7 receptor antagonist-5
    		Antagonist
    P2X7 receptor antagonist-5 (compund 13a) is a potent, orally active and long-lasting P2X7 receptor antagonist.
    P2X7 receptor antagonist-5
  • HY-148558
    P2X7 receptor antagonist-3
    		Antagonist
    P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats.
    P2X7 receptor antagonist-3
  • HY-109067
    Opiranserin
    		Antagonist
    Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin
  • HY-128891
    Eperisone
    		Antagonist
    Eperisone ((±)-Eperisone) is an antispasmodic agent and centrally acting muscle relaxant useful in the study of diseases characterized by muscle stiffness and pain. Eperisone acts by relaxing skeletal and vascular smooth muscle, resulting in vasodilation, decreased muscle tone, improved circulation, and inhibition of pain reflexes. Eperisone is also a potent P2X7 receptor antagonist.
    Eperisone
  • HY-139627
    P2X receptor-1
    		Inhibitor
    P2X receptor-1 is a potential inhibitor of P2X receptor for the research of pain and inflammation.
    P2X receptor-1
  • HY-102063
    MRS 2219
    		Agonist
    MRS 2219 (Pyridoxol) is a selective pharmacological probe of P2X1 receptor. MRS 2219 selectively potentiated ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM.
    MRS 2219
  • HY-134440A
    α,β-Methylene-ATP
    		Agonist
    α,β-Methylene-ATP is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system.
    α,β-Methylene-ATP
  • HY-153548
    P2X2/3 modulator-1
    		Modulator
    P2X2/3 modulator-1 (Compound 46) is a P2X2/3 modulator. P2X2/3 modulator-1 can be used in the study of pain, central nervous system disorders and inflammation.
    P2X2/3 modulator-1
P2X Receptor Isoform Comparison

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