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Results for "

P2X7 receptor antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Apoptosis (1) Histamine Receptor (2) P2X Receptor (19)
By Research Areas:	Cancer (3) Inflammation/Immunology (7) Neurological Disease (14)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150059

P2X7 receptor antagonist-2	P2X Receptor	Neurological Disease Inflammation/Immunology
P2X7 receptor antagonist-2 is a potent **P2X7 receptor** antagonist with a pIC₅₀ value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation .

HY-145466

EVT-401	P2X Receptor	Neurological Disease
EVT-401 (P2X7 receptor antagonist-1) is a purinergic **P2X7 receptor** antagonist. EVT-401 has efficacy of combating neuroinflammation .

HY-50697

A-740003 Maximum Cited Publications 12 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.

HY-155194

P2X7 receptor antagonist-4	Others	Inflammation/Immunology
P2X7 receptor antagonist-4 (Compound 14a) is a *P2X7R* antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC₅₀ in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice .

HY-100483

A-804598 3 Publications Verification	P2X Receptor	Cancer
A-804598 is a CNS 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-15487

CE-224535 PF-04905428	P2X Receptor	Neurological Disease
CE-224535 is a selective **P2X₇ receptor** antagonist.

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 .

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 .

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 .

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 .

HY-15488A

A 438079 hydrochloride 10+ Cited Publications	P2X Receptor	Neurological Disease
A 438079 (hydrochloride) is a potent, and selective P2X₇ *receptor* antagonist with pIC₅₀ of 6.9.

HY-15488

A 438079 10+ Cited Publications	P2X Receptor	Neurological Disease
A 438079 is a potent, and selective P2X₇ *receptor* antagonist with pIC₅₀ of 6.9.

HY-15469

GW791343 dihydrochloride	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 .

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 .

HY-123205

Oxatomide	Histamine Receptor P2X Receptor 5-HT Receptor	Inflammation/Immunology
Oxatomide is a potent and orally active dual H1-histamine receptor and **P2X7 receptor** antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC₅₀ of 0.95 μM). Oxatomide inhibits ATP-induced Ca ²⁺ influx with an IC₅₀ value of 0.43 μM and also inhibits serotonin .

HY-123205R

Oxatomide (Standard)	Histamine Receptor P2X Receptor 5-HT Receptor	Inflammation/Immunology
Oxatomide (Standard) is the analytical standard of Oxatomide. This product is intended for research and analytical applications. Oxatomide is a potent and orally active dual H1-histamine receptor and **P2X7 receptor** antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC₅₀ of 0.95 μM). Oxatomide inhibits ATP-induced Ca ²⁺ influx with an IC₅₀ value of 0.43 μM and also inhibits serotonin .

HY-117508

JNJ-54175446	P2X Receptor	Neurological Disease
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-108669

AZ10606120 dihydrochloride 1 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 .

HY-N5025

Bullatine A	P2X Receptor Apoptosis	Inflammation/Immunology Cancer
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent *P2X7* antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses . Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed .

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, K_i**s 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-B1901

Eperisone hydrochloride (±)-Eperisone hydrochloride	Others	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 .

Bullatine A	Structural Classification Alkaloids Piperidine Alkaloids Classification of Application Fields Source classification Ranunculaceae Aconitum carmichaeli Debx. Plants Inflammation/Immunology Disease Research Fields	P2X Receptor Apoptosis
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent *P2X7* antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses . Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed .

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P2X7 receptor antagonists

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