P2X receptors are a family 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 purinergic receptors. P2X receptors are present in a diverse array of organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba. seven separate genes coding for P2X subunits have been identified, and named to as P2X1 through P2X7. The pharmacology of a given P2X receptor is largely determined by its subunit makeup. Different subunits exhibit different sensitivities to purinergic agonists and antagonists. Of continuing interest is the fact that some P2X receptors (P2X2, P2X4, human P2X5, and P2X7) exhibit multiple open states in response to ATP, characterized by a time-dependent increase in the permeabilities of large organic ions and nucleotide binding dyes.


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NF 449

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[1][2].

  • CAS Number: 627034-85-9
  • MF: C41H24N6Na8O29S8
  • MW: 1505.090
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lu AF27139

Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.

  • CAS Number: 2097117-06-9
  • MF: C21H19ClF3N5O2S
  • MW: 497.9212
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NF 279

NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env[1][2].

  • CAS Number: 202983-32-2
  • MF: C49H30N6Na6O23S6
  • MW: 1401.118
  • Catalog: HIV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NF023

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[1][2][3][4].

  • CAS Number: 104869-31-0
  • MF: C35H20N4Na6O21S6
  • MW: 1162.88000
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

8-Bromo-ATP

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[1][2][3].

  • CAS Number: 23567-97-7
  • MF: C10H15BrN5O13P3
  • MW: 586.07700
  • Catalog: P2X Receptor
  • Density: 2.85g/cm3
  • Boiling Point: 1009.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 564.5ºC

Sivopixant

Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect[1].

  • CAS Number: 2414285-40-6
  • MF: C25H22ClN5O5
  • MW: 507.93
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ISO-PPADS TETRASODIUM SALT

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)[1][2].

  • CAS Number: 207572-67-6
  • MF: C14H10N3Na4O12PS2
  • MW: 599.30
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TNP-ATP sodium salt

TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats[1].

  • CAS Number: 61368-63-6
  • MF: C16H13N8O19P34-
  • MW: 714.24
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: 1097.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 617.7ºC

NP-1815-PX

NP-1815-PX is a potent and selective P2X4R antagonist. NP-1815-PX has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions[1][2][3].

  • CAS Number: 1239578-79-0
  • MF: C21H14N4O3S
  • MW: 402.43
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P2X7-IN-2

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[1].

  • CAS Number: 1058709-63-9
  • MF: C22H21F4N3O2
  • MW: 435.41
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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].

  • CAS Number: 180064-38-4
  • MF: C9H12N2O7P2
  • MW: 322.14800
  • Catalog: Apoptosis
  • Density: 1.973 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P2X3 antagonist 37

P2X3 antagonist 37 is a potent P2X3 receptor antagonist with an IC50 of 32.45 nM for hP2X3 (WO2021115225A1, example 68)[1].

  • CAS Number: 2649318-40-9
  • MF: C18H9F4N7O2
  • MW: 431.30
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P2X3 antagonist 36

P2X3 antagonist 36 is a P2X3 antagonist extracted from patent WO2019081343A1 compound 156[1].

  • CAS Number: 2310263-59-1
  • MF: C20H18ClF3N6O3
  • MW: 482.84
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P2X7 receptor antagonist-2

P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC50 value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation[1].

  • CAS Number: 851269-75-5
  • MF: C19H18Cl2N2O2
  • MW: 377.264
  • Catalog: P2X Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 640.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 340.9±31.5 °C

Gefapixant citrate

Gefapixant citrate 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 citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].

  • CAS Number: 2310299-91-1
  • MF: C20H27N5O11S
  • MW: 545.52
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A-740003

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.

  • CAS Number: 861393-28-4
  • MF: C26H30N6O3
  • MW: 474.555
  • Catalog: P2X Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD9056 hydrochloride

AZD9056 is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.

  • CAS Number: 345303-91-5
  • MF: C24H36Cl2N2O2
  • MW: 455.46100
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZ10606120 dihydrochloride

AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth[1].

  • CAS Number: 607378-18-7
  • MF: C25H36Cl2N4O2
  • MW: 495.485
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 804598

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay. [1]In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. [2]

  • CAS Number: 1125758-85-1
  • MF: C19H17N5
  • MW: 315.37200
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JNJ-54175446

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

  • CAS Number: 1627902-21-9
  • MF: C18H13ClF4N6O
  • MW: 440.78
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW791343 trihydrochloride

GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). IC50 value: 7 (pIC50)Target: P2X7 in vitro: In cells expressing human P2X7 receptors, GW 791343 inhibits agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer. In NaCl buffer, GW 791343 reduces the maximal response to both ATP and BzATP, but there is little effect on agonist potency except for a decrease in the presence of 300–1000 nM GW 791343. GW 791343 also reduces maximal responses to ATP and BzATP in sucrose buffer, although this effect is more marked when using ATP as agonist. In sucrose buffer, GW 791343 produces a slight decrease in ATP potency at 300 nM. GW 791343 decreases BzATP potency at concentrations of 300 nM to 10 μM. A more marked increase in agonist effect is observed when using ATP as agonist in NaCl buffer with GW791343 increasing the pEC50 and maximal response to ATP at concentrations of 10 and 30 μM. In sucrose buffer, GW791343 also increases responses when using ATP as agonist [1]. GW791343 inhibits responses at the human–rat chimeric receptor in both sucrose and NaCl buffer. GW791343 increases responses to BzATP at the F95L mutant receptor [2]. GW791343 is a non-competitive antagonist and negative allosteric modulator at the human P2X7 receptor; however, GW 791343 also acts as a positive allosteric modulator at the rat P2X7 receptor [3]. At the dog P2X7 receptor, GW 791343 is an antagonist with similar potency to that determined at the human receptor [4].

  • CAS Number: 309712-55-8
  • MF: C20H27Cl3F2N4O
  • MW: 483.81000
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P2X3 antagonist 38

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[1].

  • CAS Number: 2545974-71-6
  • MF: C22H25F3N6O3
  • MW: 478.47
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY-1797

BAY-1797 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[1].

  • CAS Number: 2055602-83-8
  • MF: C20H17ClN2O4S
  • MW: 416.88
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Opiranserin hydrochloride

Opiranserin (VVZ-149) hydrochloride, 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 hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain[1][2][3].

  • CAS Number: 1440796-75-7
  • MF: C21H35ClN2O5
  • MW: 430.97
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

α,β-Methylene-ATP dilithium

α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand[1]. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7[2].

  • CAS Number: 104809-20-3
  • MF: C11H18Li2N5O12P3
  • MW: 519.09
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gefapixant

Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

  • CAS Number: 1015787-98-0
  • MF: C14H19N5O4S
  • MW: 353.397
  • Catalog: P2X Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 606.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 320.5±34.3 °C

Filapixant

Filapixant is a purinoreceptor antagonist extracted from patent WO2016091776A1, example 348. Filapixant is the active reference substance of Eliapixant[1].

  • CAS Number: 1948232-63-0
  • MF: C24H26F3N5O3S
  • MW: 521.56
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 438079

A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

  • CAS Number: 899507-36-9
  • MF: C13H9Cl2N5
  • MW: 306.15
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CE-224535

CE-224535 is a selective P2X7 receptor antagonist.

  • CAS Number: 724424-43-5
  • MF: C22H29ClN4O6
  • MW: 480.94
  • Catalog: P2X Receptor
  • Density: 1.47g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

α,β-Methylene-ATP

α,β-Methylene ATP, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7[1][2].

  • CAS Number: 7292-42-4
  • MF: C11H18N5O12P3
  • MW: 505.20800
  • Catalog: P2X Receptor
  • Density: 2.5g/cm3
  • Boiling Point: 968.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 539.3ºC