A-740003

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.

Product Specifications

CAS Number

[861393-28-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/a-740003.html

Purity

99.61

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

N#C/N=C(NC(NC(CC1=CC(OC)=C(C=C1)OC)=O)C(C)(C)C)\NC2=CC=CC3=NC=CC=C23

Molecular Formula

C26H30N6O3

Molecular Weight

474.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Grol MW, et al. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 2012 Mar 1;302 (5) :E561-75.|[2]Kim JE, et al. P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. J Neuroinflammation. 2011 Jun 2;8:62.|[3]Donnelly-Roberts DL, et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.Br J Pharmacol. 2009 Aug;157 (7) :1203-14. Epub 2009 Jun 22.|[4]Honore P, et al. A-740003 [N- (1-{[ (cyanoimino) (5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl) -2- (3,4-dimethoxyphenyl) acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Ther. 2006 Dec;319 (3) :1376-85. Epub 2006 Sep 18.|[5]Y. H. Gao, et al. Effect of electroacupuncture on the cervicospinal P2X7 receptor/fractalkine/CX3CR1 signaling pathway in a rat neck-incision pain model. Purinergic Signal. 2017 Jun;13 (2) :215-225.