1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. P2X7 Receptor Isoform
  5. P2X7 Receptor Antagonist

P2X7 Receptor Antagonist

P2X7 Receptor Antagonists (18):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-15488
    A 438079
    Antagonist 99.88%
    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • 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.
  • HY-183784
    P2X7R antagonist-1
    Antagonist
    P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research.
  • HY-179373
    UB-MBX-46
    Antagonist
    UB-MBX-46 is a potent and selective P2X7 receptor antagonist with IC50s of 0.514 nM (hP2X7R), 40.6 nM (rP2X7R), and 4.52 nM (mP2X7R), respectively. UB-MBX-46 interacts with the classical allosteric pocket of the human P2X7 receptor. UB-MBX-46 can be used for cancer, atherosclerosis, and neurode generation research.
  • HY-15488A
    A 438079 hydrochloride
    Antagonist 99.99%
    A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
  • HY-101418
    JNJ-47965567
    Antagonist 99.79%
    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.
  • HY-108669
    AZ10606120 dihydrochloride
    Antagonist 99.93%
    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
  • HY-100483
    A-804598
    Antagonist 98.68%
    A-804598 is a BBB penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
  • HY-123205
    Oxatomide
    Antagonist 98.11%
    Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.
  • HY-123857
    JNJ-55308942
    Antagonist 99.92%
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
  • HY-117508
    JNJ-54175446
    Antagonist 99.30%
    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.
  • HY-15487
    CE-224535
    Antagonist 98.91%
    CE-224535 is a selective P2X7 receptor antagonist.
  • HY-13954
    A 839977
    Antagonist 98.74%
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-132981
    Lu AF27139
    Antagonist 99.71%
    Lu AF27139 is a potent, selective, and orally active 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 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
  • HY-145466
    EVT-401
    Antagonist 99.89%
    EVT-401 (P2X7 receptor antagonist-1) is a purinergic P2X7 receptor antagonist. EVT-401 has efficacy of combating neuroinflammation.
  • 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.
  • HY-175196
    P2X7 receptor antagonist-6
    Antagonist
    P2X7 receptor antagonist-6 (Compound 2g) is a negative allosteric P2X7 receptor antagonist with an IC50 of 1.31  μM for hP2X7. P2X7 receptor antagonist-6 can be used for cancer, neurodegenerative, inflammatory, and infectious diseases research.