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P2X Receptor

The ATP-gated P2X receptor cation channel family, or simply P2X receptor family, consists of cation-permeable ligand-gated ion channels that open in response to the binding of extracellular adenosine 5'-triphosphate (ATP). They belong to a larger family of receptors known as the ENaC/P2X superfamily. ENaC and P2X receptors have similar 3-D structures and are homologous. P2X receptors are present in a diverse array of organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba.

  • BzATP triethylammonium salt
    TP2226112898-15-4
    BzATP triethylammonium salt is a P2X7 receptor agonist.
    • $41
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  • CI 75300
    T863594875-80-6
    CI 75300 targets the P2X purinoceptor 7 (human).
    • $50
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  • CTP disodium dihydrate
    T788181012-87-5
    CTP disodium dihydrate is an agonist of P2X4 purinergic receptor
    • $50
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  • AZ 11645373
    T21659227088-94-0
    AZ 11645373 (3-[1-[[(3'-NITRO[1,1'-BIPHENYL]-4-YL)OXY]METHYL]-3-(4-PYRIDINYL)PROPYL]-2,4-THIAZOLIDINEDIONE) is a highly selective and potent human P2X7 receptor antagonist that has no effect on mouse/rat P2X7 receptor.
    • $132
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  • AZ10606120 dihydrochloride
    T14366607378-18-7In house
    AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.
    • $61
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  • (E/Z)-Sivopixant
    T96531640808-39-4In house
    (E/Z)-Sivopixant ((E/Z)-S-600918)is a potent P2X3 receptor antagonist, IC50 = 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.
    • $88
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  • 5-(N,N-Hexamethylene)-amiloride
    T46991428-95-1In house
    5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative, shown to inhibit TRPA1-mediated calcium signal (IC50: 35 μM). It is an inhibitor of the Na+/H+ exchanger (NHE), with Ki of 0.013-2.4 μM for various NHE isoforms. 5-HMA also blocks ASIC3 channels by 51% at 20 μM.
      7-10 days
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    • JNJ-54175446
      T156221627902-21-9In house
      JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β/IL-18 from microglia, and may be used in the study of depression.
      • $293
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    • Oxatomide
      T1983960607-34-3In house
      Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.
      • $32
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    • JNJ-55308942
      T378062166558-11-6In house
      JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.
      • $70
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    • JNJ-42253432
      T276831428327-35-8In house
      JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.
      • $118
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    • A-804598
      T36391125758-85-1
      A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).
      • $23
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    • KN-62
      T2694127191-97-3
      KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.
      • $30
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    • Sivopixant
      T400452414285-40-6
      Sivopixant (S-600918) (S-600918) is a potent and selective antagonist of P2X3 receptor (P2X3 IC 50 =4.2 nM; P2X2/3 IC 50 =1100 nM). Sivopixant shows strong analgesic effect .
      • $148
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    • Bongkrekic acid
      T3606711076-19-0
      Bongkrekic acid (Bongkrekic Acid (ammonium salt)) is a mitochondrial toxin secreted by Burkholderia gladioli that inhibits adenine nucleotide translocase (ANT).Bongkrekic acid Bongkrekic acid Bongkrekic acid induces extracellular traps in neutrophils through signaling mediated by p38, ERK, PAD4, and P2X1.
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    • A-740003
      T3690861393-28-4
      A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18/40 nM, for rat/human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice.
      • $34
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    • JNJ-47965567
      T42981428327-31-4
      JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).
      • $34
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    • A 438079 hydrochloride
      T2673899431-18-6
      A 438079 hydrochloride (A-438079 HCl) is a potent and selective P2X7 receptor antagonist with pIC50 of 6.9.
      • $41
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    • BX430
      T14844688309-70-8
      BX430 is used for chronic pain and cardiovascular disease and it is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity.
      • $39
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    • Oxidized ATP trisodium salt
      T7863971997-40-5
      Oxidized ATP trisodium salt (oATP) is a broad-spectrum inhibitor of P2 receptors, irreversibly antagonizing P2X7R activation and inhibiting c-reactive protein (CRP)-induced NLRP3 inflammasome activation. It is utilized in atherosclerosis research [1] [2].
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    • Indophagolin
      T89461207660-00-1
      Indophagolin is a potent, indoline-containing autophagy inhibitor with IC50 of 140 nM. Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively.
      • $89
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    • Opiranserin hydrochloride
      T98331440796-75-7
      Opiranserin (VVZ-149) hydrochloride 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. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.
      • $97
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    • PSB-12062
      T1256855476-47-6
      PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine) is a potent and selective antagonist of P2X4(IC50 of 1.38 μM for human P2X4).
      • $30
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    • Gefapixant
      T50991015787-98-0
      Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
      • $38
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    • NP-1815-PX
      T711551239578-80-3
      NP-1815-PX is a selective P2X4R antagonist with demonstrated anti-inflammatory effects and the capability to alleviate pain in chronic pain models. Additionally, it impedes contractions of guinea pig tracheal and bronchial smooth muscle (TSM and BSM)[1][2][3].
      • $1,520
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    • AF-353
      T2087865305-30-2
      AF-353 (Ro-4), an effective and orally bioavailable antagonist of the P2X3/P2X2/3 receptor, inhibits human and rat P2X3 (pIC50= 8.0).
      • $31
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    • BAY-1797
      T104662055602-83-8
      BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.
      • $34
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    • Lappaconitine
      T280632854-75-4
      Lappaconitine ((+)-Lappaconitine), isolated from Aconitum sinomontanum Nakai, was characterized as an analgesic.
      • $40
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    • Opiranserin
      T163991441000-45-8
      Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).
      • $1,520
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    • P2X3-IN-1
      T786062823331-49-1
      P2X3-IN-1 (example 7) is a P2X3 receptor inhibitor suitable for research on neurogenic diseases [1].
      • $1,370
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    • P2X3 antagonist 38
      T791152545974-71-6
      Compound 38, also known as Compound 4, is a potent, orally active P2X3 antagonist that demonstrates inhibitory activity with IC50 values of 0.132 µM, 0.165 µM, and 0.421 µM against human (hP2X3), rat (rP2X3), and guinea pig (gpP2X3) P2X3 receptors, respectively [1].
      • $1,670
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    • Ivermectin
      T113170288-86-7
      Ivermectin (MK-933) is a glutamate-gated chloride channel (GluCls) activator, with antiparasitic activity.
      • $32
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    • CE-224535
      T14920724424-43-5
      CE-224535 (PF-04905428) is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.
      • $127
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    • AZD9056 hydrochloride
      T14385345303-91-5
      AZD9056 hydrochloride is a P2X7 inhibitor,Which plays a significant role in pain-causing diseases and inflammation.
      • $39
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    • α,β-Methylene ATP trisodium
      T135411343364-54-4
      α,β-Methylene ATP trisodium, a phosphonate analog of ATP, is a selective P2X agonist that induces enhanced contraction of UBSM. α,β-Methylene ATP trisodium inhibits P2X1 and P2X3, but is inactive against P2X2, 4 and 7.
      • $1,650
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    • PPADS tetrasodium
      T16564192575-19-2
      PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.
      • $49
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    • Lu AF27139
      T97862097117-06-9
      Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.
      • $93
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    • GW791343 trihydrochloride
      T6526309712-55-8
      GW791343 trihydrochloride (GW791343 3HCl) is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
      • $72
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    • Bullatine A
      T4S05361354-84-3
      1. Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects, may be used for the treatment of neurodegenerative diseases such as arthritis.
      • $33
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    • RO-3
      T55131026582-88-6
      RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor
      • $48
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    • A 839977
      T14076870061-27-1
      A 839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic activity that inhibits BzATP-induced calcium efflux from the P2X7 receptor for the study of renal fibrosis.
      • $37
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    • GW791343 dihydrochloride
      T78051019779-04-4
      GW791343 dihydrochloride (GW791343 (HCl)) is a P2X7 allosteric modulator.
      • $39
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    • A 438079
      T10207899507-36-9
      A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9).
      • $41
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    • GSK-1482160
      T610251001389-72-5
      GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.
      • $48
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    • Eliapixant
      T95191948229-21-7
      Eliapixant (BAY 1817080) (BAY 1817080) is a potent and selective P2X3 receptor antagonist, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.
      • $135
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    • Minodronic acid
      T8436180064-38-4
      Minodronic acid(YM-529) is a P2X2/3 receptor antagonist with anticancer activity, directly or indirectly inhibiting the proliferation of cancer cells and inducing apoptosis. Minodronic acid has been shown to inhibit the metastasis of various types of cancer cells.Minodronic-acid has been used in the study of osteoporosis.
      • $30
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    • NF023 hexasodium
      TP2272104869-31-0
      NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively.
      • $448
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    • Brilliant blue G-250
      T207316104-58-1
      Brilliant blue G-250 (Acid blue 90, Coomassie Brilliant Blue G) is an antagonist of the P2X7 purinergic receptor.
      • $35
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    • Camlipixant
      T678851621164-74-6
      Camlipixant (BLU-5937) is an orally active purine P2X3 receptor antagonist that is potent, selective and competitive. camlipixant has an IC50 of 25 nM for the hP2X3 homotrimer. camlipixant can be used for the treatment of respiratory disorders and Camlipixant has a strong cough suppressant effect.
      • $97
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    • ATP disodium salt
      T1352987-65-5
      ATP disodium salt (Adenosine-Triphosphate) is a P2 purinoceptor agonist.
      • $50
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