p2x7r

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.

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.

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

A 438079 is a potent and selective antagonist of the P2X7 receptor (pIC50: 6.9).

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.

CE-224535 (PF-04905428) is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.

P2X7 receptorantagonist-6 (Compound 2g) is a negative allosteric antagonist of the P2X7 receptor, which shows an IC50 of 1.31 μM against hP2X7. This compound is applicable in the study of cancer, neurodegenerative diseases, inflammation, and infectious diseases.

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

P2X7 receptor antagonist-2 is a highly potent inhibitor of the P2X7 receptor, with a pIC50 value range of 6.5-7.5 and demonstrated efficacy in combating neuroinflammation [1].

P2X7 receptor antagonist-1 is a purinergic P2X7 receptor antagonist with anti-neuroinflammatory effects.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

GW791343 dihydrochloride (GW791343 (HCl)) is a P2X7 allosteric modulator.

Zeaxanthin dipalmitate (Physalien) is a lutein carotenoid found in fruits with anti-inflammatory, hepatoprotective, and anti-oxidative stress activity that attenuates ethanol-induced liver injury.Zeaxanthin dipalmitate restores mitochondrial autophagy, a function that has been inhibited by ethanol intoxication. Zeaxanthin dipalmitate protects degenerated photoreceptors in the retina of mice and improves visual acuity in a mouse model of photoreceptor degeneration, and may be used in studies of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).

SMW139 is a selective allosteric antagonist of the P2X7 receptor, exhibiting a Ki value of 32 nM for human P2X7R. In rat liver microsomes, its half-life is 47 minutes. SMW139 is applicable in research related to inflammation, Alzheimer's disease, and multiple sclerosis.

Oxidized ATP trisodium salt (oATP) is a broad-spectrum P2 receptor inhibitor that irreversibly antagonizes P2X7R activation and inhibits CRP-induced NLRP3 inflammasome activation, making it useful in atherosclerosis research [1] [2].

HEI3090 is an activator of the P2X7R receptor. This compound enhances the production of IL-18 by stimulating dendritic cells that express P2X7R, which in turn promotes the production of IFN-γ by natural killer cells and CD4T cells within tumors, triggering a sustained anti-tumor response. Additionally, HEI3090 can be used to improve the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC).