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-136254
    BzATP triethylammonium salt
    		Agonist 99.19%
    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-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 Gsα-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-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-50697
    A-740003
    		Antagonist 99.61%
    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-15488
    A 438079
    		Antagonist 99.88%
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079
  • HY-186112
    PSFL2915
    		Inhibitor 98.72%
    PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2. PSFL2915 exhibits ~42-fold selectivity over human P2X2. PSFL2915 can be used for the research of chronic cough.
    PSFL2915
  • HY-182715
    PSB-10211
    		Antagonist
    PSB-10211 is a P2X2 receptor antagonist with an IC50 of 0.086 μM against rat P2X2 receptors. PSB-10211 inhibits ATP-mediated currents of rat P2X2 receptors expressed in Xenopus oocytes. PSB-10211 can be used in studies related to pain and urinary incontinence.
    PSB-10211
  • HY-182642
    MRS2339
    		Activator
    MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R. MRS2339 induces ionic currents via P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy.
    MRS2339
  • 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-101911
    5-BDBD
    		Antagonist 99.94%
    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-101044
    PPADS tetrasodium
    		Antagonist 99.9%
    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-P0170
    TB500
    		Agonist 99.57%
    TB500 is a synthetic version of an active region of thymosin β4. TB500 exhibits anti-fibrotic and wound healing activities by inhibiting the Akt signaling pathway and binding to actin. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation.
    TB500
  • HY-13290
    KN-62
    		Antagonist 99.00%
    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-108652
    α,β-Methylene-ATP trisodium
    		Agonist 99.0%
    α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium 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 trisodium 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 trisodium 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 trisodium
  • HY-130605
    BAY-1797
    		Antagonist 99.76%
    BAY-1797, a chemical probe, 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-15488A
    A 438079 hydrochloride
    		Antagonist 99.99%
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 hydrochloride
  • HY-101588
    Gefapixant
    		Antagonist 99.93%
    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-19427A
    AZD9056 hydrochloride
    		Inhibitor 98.18%
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
    AZD9056 hydrochloride
  • HY-101418
    JNJ-47965567
    		Antagonist 99.87%
    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-113273A
    Diadenosine pentaphosphate pentasodium
    		Inhibitor 99.13%
    Diadenosine pentaphosphate pentasodium is an agonist and negative modulator of the P2X1 receptor, an endogenous vasoactive purine dinucleotide that can be isolated from platelets. Diadenosine pentaphosphate pentasodium mediates negative regulation of dendrite growth and number by activating homologous and heterologous P2X1 receptors, which triggers a transient and moderate increase in intracellular calcium levels within dendritic growth cones. Diadenosine pentaphosphate pentasodium is widely present in secretory vesicles such as platelets, chromaffin cells and brain synaptosomes, and exhibits selective activity on dendrite growth of cultured hippocampal neurons, inhibiting only dendrite growth without affecting axon growth. Diadenosine pentaphosphate pentasodium has a weaker ability to compete with RcCHAD for binding to polyP than short-chain polyPs.
    Diadenosine pentaphosphate pentasodium
P2X Receptor Isoform Comparison

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