P2X7 Receptor Antagonist

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

KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a K_i 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.

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.

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

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pK_is 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.

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.

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.

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.

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.

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.

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.

CE-224535 is a selective P2X₇ receptor antagonist.

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC₅₀s of 12 and 2.4 nM for human and rat, K_is 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.

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.

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.

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.