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Results for "

human P2X7 receptor

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50697
    A-740003
    Maximum Cited Publications
    17 Publications Verification

    		 P2X Receptor Neurological Disease
    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-108669
    AZ10606120 dihydrochloride
    2 Publications Verification

    		 P2X Receptor Neurological Disease Cancer
    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 .
    AZ10606120 dihydrochloride
  • HY-B1901
    Eperisone hydrochloride

    (±)-Eperisone hydrochloride

    		 P2X Receptor Neurological Disease
    Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
    Eperisone hydrochloride
  • HY-100483
    A-804598
    3 Publications Verification

    		 P2X Receptor Neurological Disease Cancer
    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 .
    A-804598
  • HY-13954
    A 839977
    1 Publications Verification

    		 P2X Receptor Neurological Disease Inflammation/Immunology
    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 .
    A 839977
  • HY-132981
    Lu AF27139

    		P2X Receptor Neurological Disease
    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 .
    Lu AF27139
  • HY-B1901R
    Eperisone hydrochloride (Standard)

    (±)-Eperisone hydrochloride (Standard)

    		 P2X Receptor Reference Standards Neurological Disease
    Eperisone (hydrochloride) (Standard) is the analytical standard of Eperisone (hydrochloride). This product is intended for research and analytical applications. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
    Eperisone hydrochloride (Standard)
  • HY-19888
    GSK-1482160

    		P2X Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .
    GSK-1482160
  • HY-15469
    GW791343 dihydrochloride
    1 Publications Verification

    		 P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
    GW791343 dihydrochloride
  • HY-108670
    AZ 11645373

    		P2X Receptor Inflammation/Immunology
    AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM .
    AZ 11645373
  • HY-15470
    GW791343 trihydrochloride

    		P2X Receptor Neurological Disease
    GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
    GW791343 trihydrochloride
  • HY-179373
    UB-MBX-46

    		P2X Receptor Cardiovascular Disease Neurological Disease Cancer
    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 .
    UB-MBX-46
  • HY-148558
    P2X7 receptor antagonist-3

    		P2X Receptor Neurological Disease
    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 .
    P2X7 receptor antagonist-3
  • HY-124300
    JNJ-54166060

    		P2X Receptor Others
    JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively .
    JNJ-54166060
  • HY-171462
    SMW139

    		P2X Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    SMW139 is a selective allosteric antagonist of P2X7 receptor, with a Ki value of 32 nM for human P2X7R. The half-life of SMW139 in rat liver microsomes is 47 minutes. SMW139 can be used for inflammation, Alzheimer’s disease, multiple sclerosis study .
    SMW139
  • HY-123382
    GSK-1482160 (isomer)

    		Drug Isomer Neurological Disease Inflammation/Immunology
    GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
    GSK-1482160 (isomer)
  • HY-165557
    GSK1370319A

    		P2X Receptor Inflammation/Immunology
    GSK1370319A (compound 1a) is a human P2X7 receptor inhibitor with an IC50 of 474 nM and a Ki of 176 nM. GSK1370319A inhibits the production of IL-1β, reduces the generation of reactive oxygen species (ROS), and increases the survival rate of macrophages. GSK1370319A can be used for the research of inflammatory bowel disease .
    GSK1370319A
  • HY-108669R
    AZ10606120 dihydrochloride (Standard)

    		Reference Standards P2X Receptor Neurological Disease Cancer
    AZ10606120 dihydrochloride (Standard) is the analytical standard of AZ10606120 (dihydrochloride) (HY-108669). This product is intended for research and analytical applications. 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 .
    AZ10606120 dihydrochloride (Standard)
  • HY-186112
    PSFL2915

    		P2X Receptor Inflammation/Immunology
    PSFL2915 is a 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, and exhibits ~42-fold selectivity for human P2X3 over human P2X2. PSFL2915 inhibits human P2X3 activation by preventing allosteric tightening of the inner pocket of the head domain required for channel opening, with magnesium-dependent inhibition. PSFL2915 inhibits rat P2X2/3 and human P2X2 receptor activation, and has low activity against human P2X1, P2X4, and P2X7 receptors. PSFL2915 can be used for the research of chronic cough .
    PSFL2915
  • HY-108670R
    AZ 11645373 (Standard)

    		Reference Standards P2X Receptor Inflammation/Immunology
    AZ 11645373 (Standard) is the analytical standard of AZ 11645373 (HY-108670). This product is intended for research and analytical applications. AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM .
    AZ 11645373 (Standard)
  • HY-183784
    P2X7R antagonist-1

    		P2X Receptor FAK MMP Cancer
    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 .
    P2X7R antagonist-1

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