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Isoforms Recommended:	P2X7 Receptor

Results for "

P2X7 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Adiponectin Receptor (1) Angiotensin Receptor (1) Apoptosis (1) Autophagy (1) CaMK (1) Gap Junction Protein (1) Histamine Receptor (2) Interleukin Related (2) NOD-like Receptor (NLR) (1) P2X Receptor (35)
By Research Areas:	Cancer (8) Cardiovascular Disease (3) Inflammation/Immunology (16) Metabolic Disease (1) Neurological Disease (16)

Inhibitors & Agonists

Peptides

Natural
Products

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-19888

GSK-1482160	P2X Receptor	Inflammation/Immunology
GSK-1482160 is an orally available negative allosteric modulator of the *P2X7* receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .

HY-18725A

P2X7-IN-2 TFA	P2X Receptor Interleukin Related	Cardiovascular Disease Inflammation/Immunology
P2X7-IN-2 TFA (compound 58) is a *P2X7* receptor inhibitor. P2X7-IN-2 TFA inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 TFA can be used for the research of autoimmunity, inflammation and cardiovascular disease .

HY-50697

A-740003 Maximum Cited Publications 15 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-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-162951

P2X7 receptor antagonist-5	P2X Receptor	Cancer
P2X7 receptor antagonist-5 (compund 13a) is a potent, orally active and long-lasting *P2X7* receptor antagonist .

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-18725

P2X7-IN-2	P2X Receptor Interleukin Related	Cardiovascular Disease Inflammation/Immunology
P2X7-IN-2 (compound 58) is a *P2X7* receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease .

HY-124300

JNJ-54166060	P2X Receptor	Others
JNJ-54166060 is a potent and selective **P2X7 receptor antagonist, with IC₅₀*s of 4/115/72 nM for human/rat/mouse P2X7* receptor, respectively .

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-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-15487

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

HY-136254

BzATP triethylammonium salt 5+ Cited Publications	P2X Receptor	Inflammation/Immunology Cancer
BzATP triethylammonium salt acts as a P2X receptor agonist with pEC₅₀s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively . BzATP triethylammonium salt is potent at P2X7 receptors with EC₅₀s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively .

HY-18745

BzATP triethylammonium Benzoylbenzoyl-ATP triethylammonium	P2X Receptor	Inflammation/Immunology Cancer
BzATP triethylammonium acts as a P2X receptor agonist with pEC₅₀s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively . BzATP triethylammonium is potent at P2X7 receptors with EC₅₀s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively .

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-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-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-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-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-19427

AZD9056	P2X Receptor	Cancer
AZD9056 is a **P2X7 purinergic receptor** antagonist with anticancer activity. AZD9056 can inhibit the invasion and metastasis of cancer stem cells .

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-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 .

HY-117508

JNJ-54175446	P2X Receptor	Neurological Disease
JNJ-54175446 is a potent and selective brain penetrant **P2X7 receptor antagonist, with pIC₅₀*s of 8.46 and 8.81 for hP2X7 receptor* and rP2X7 receptor, respectively.

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 .

HY-122282

AZ11657312	Angiotensin Receptor	Cardiovascular Disease
AZ11657312 is a P2X7 receptor antagonist with activity to restore stress natriuresis. AZ11657312 significantly increased renal medullary perfusion, only in mice treated with angiotensin II. AZ11657312 improves tissue oxygenation by blocking P2X7R, especially in areas of the kidney that are underoxygenated. Administration of AZ11657312 increased sodium excretion up to sixfold while normalizing blood pressure .

HY-N1478

Gardenoside 1 Publications Verification	P2X Receptor	Neurological Disease
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis .

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-128891

Eperisone	P2X Receptor	Neurological Disease
Eperisone ((±)-Eperisone) is an antispasmodic agent and centrally acting muscle relaxant useful in the study of diseases characterized by muscle stiffness and pain. Eperisone acts by relaxing skeletal and vascular smooth muscle, resulting in vasodilation, decreased muscle tone, improved circulation, and inhibition of pain reflexes. Eperisone is also a potent *P2X7* receptor antagonist .

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-134440A

α,β-Methylene-ATP	P2X Receptor	Inflammation/Immunology
α,β-Methylene ATP, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .

HY-13290

KN-62 5+ Cited Publications	CaMK P2X Receptor	Metabolic Disease Cancer
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.

HY-108652

α,β-Methylene-ATP trisodium	P2X Receptor	Inflammation/Immunology
α,β-Methylene-ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand . α,β-Methylene-ATP trisodium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .

HY-134440

α,β-Methylene-ATP dilithium	P2X Receptor	Inflammation/Immunology
α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand . α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7 .

HY-P1137

10Panx	Gap Junction Protein	Others
10Panx is a biological active peptide. (This is a Pannexin-1 (Panx1) mimetic blocking peptide. Pannexin-1 is a recently identified membrane protein that can form gap junction-like connections allowing intercellular passage of dyes when overexpressed in two adjacent oocytes or mammalian epithelial cell lines. Blockade of pannexin-1 in macrophage endogenously expressing the ATP-gated P2X7 receptor (P2X7R) blocks the initial dye uptake, but not the ionic current, and also blocks processing and release of interleukin-1b (IL-1b) in response to P2X7R activation.)

HY-N9182

Zeaxanthin dipalmitate Physalien	Adiponectin Receptor P2X Receptor Autophagy	Inflammation/Immunology
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with **p2X7 receptor (K_d=81.2 nM) and adiponectin receptor 1 (AdipoR1; K_d=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy** functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .

HY-137888A

Oxidized ATP trisodium salt oATP trisodium salt	P2X Receptor NOD-like Receptor (NLR)	Inflammation/Immunology
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes *P2X7R* activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis .

Cat. No.	Product Name	Target	Research Area

HY-P1137

10Panx	Gap Junction Protein	Others
10Panx is a biological active peptide. (This is a Pannexin-1 (Panx1) mimetic blocking peptide. Pannexin-1 is a recently identified membrane protein that can form gap junction-like connections allowing intercellular passage of dyes when overexpressed in two adjacent oocytes or mammalian epithelial cell lines. Blockade of pannexin-1 in macrophage endogenously expressing the ATP-gated P2X7 receptor (P2X7R) blocks the initial dye uptake, but not the ionic current, and also blocks processing and release of interleukin-1b (IL-1b) in response to P2X7R activation.)

Gardenoside 1 Publications Verification	Structural Classification Iridoids Terpenoids Source classification Rubiaceae Plants Gardenia jasminoides Ellis	P2X Receptor
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis .

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 .

Zeaxanthin dipalmitate Physalien	Classification of Application Fields Terpenoids Source classification Diterpenoids Plants Solanaceae Lycium chinense Miller Disease Research Fields Inflammation/Immunology	Adiponectin Receptor P2X Receptor Autophagy
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with **p2X7 receptor (K_d=81.2 nM) and adiponectin receptor 1 (AdipoR1; K_d=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy** functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .

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P2X7 receptor

Inhibitors & Agonists

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