P2X Receptor

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  1. P2X7 modulator

    GW791343 HCl acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.
  2. P2X7 receptor antagonist

    A 740003 is a novel competitive antagonist of P2X7 receptors (IC50 values = 40 nM for human and 18 nM for rat).
  3. Ticlopidine is an adenosine diphosphate (ADP) receptor inhibitor. It inhibits platelet aggregation by altering the function of platelet membranes by blocking ADP receptors. This prevents the conformational change of glycoprotein IIb/IIIa which allows platelet binding to fibrinogen.
  4. P2X1 antagonist

    NF279 is a suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB ~ 1 μM in smooth muscle).
  5. P2X3 and P2X2/3 receptor antagonist

    A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
  6. P2X7 receptor antagonist

    A-438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 uM).
  7. P2X3/P2X2/3 receptor antagonist

    AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).
  8. P2X7 receptor antagonist

    A 438079 Hcl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).
  9. hepatoprotective agent

    Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
  10. P2X7 receptor antagonist

    A-804598 is a P2X7 selective, competitive antagonist with the IC50s value for human, rat and mouse channels of 11, 10 and 9 nM, respectively.
  11. P2X7 receptor antagonist

    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.
  12. P2X3R antagonist

    Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
  13. P2X4 antagonist

    PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
  14. P2X7R antagonist

    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10?nM.
  15. P2X7 selective antagonist

    A 839977 is a P2X7 selective antagonist.
  16. P2X7 receptor antagonist

    CE-224535 is a selective P2X7 receptor antagonist.
  17. P2X7 allosteric modulator

    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).
  18. purinergic P2X2/3 receptors antagonist

    Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.

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