Home Neuronal Signaling P2 Receptor antagonist A-804598 For research use only.

A-804598

A-804598 is a selective P2X7R antagonist with high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors.

A-804598 Chemical Structure

A-804598 Chemical Structure

CAS No. 1125758-85-1

Purity & Quality Control

Batch: S872501 DMSO]63 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.03%
99.03

A-804598 Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Biological Activity

Description A-804598 is a selective P2X7R antagonist with high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors.
Targets
rat P2X7R [1] rat P2X7R [1] human P2X7R [1]
9 nM 10 nM 11 nM
In vitro
In vitro A-804598 represents a structurally novel, competitive, and selective antagonist that has equivalent high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. A-804598 also potently blocks agonist stimulated release of IL-1β(IC50 of 8.5 nM) and Yo-Pro uptake (IC50 of 8.1 nM) from differentiated THP-1 cells that natively express human P2X7 receptors. Although A-840598 potently blocks P2X7 receptor activation, at concentrations up to 100 μM, it does not significantly reduce agonist-evoked changes in intracellular calcium concentrations mediated by a variety of other P2X and P2Y receptors. A-840598 shows weak or no activity for interating with a large array of G-protein-coupled receptors, enzymes, transporters, and ion channels (CEREP, Poitiers, France)(IC50 > 5-10 μM)[1].
Cell Research Cell lines SOD1-G93A primary microglia
Concentrations 10 μM
Incubation Time 15 min or 1 h
Method

SOD1-G93A microglia are treated with 300 μM BzATP or 3 mM ATP for 15 min or 1 h with or without 10 μM A-804598 and subjected to western blotting and immunoreactions with anti-p-mTOR and anti-mTOR or anti-GAPDH.
In Vivo
In vivo Inhibition of P2X7 through the antagonist A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord[2].
Animal Research Animal Models SOD1-G93A mice
Dosages 30 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 315.37 Formula

C19H17N5
CAS No. 1125758-85-1 SDF --
Smiles CC(C1=CC=CC=C1)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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