A-804598

Catalog No.S8725

For research use only.

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

CAS No. 1125758-85-1

Selleck's A-804598 has been cited by 3 Publications

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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

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].

In vivo Inhibition of P2X7 through the antagonist A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord[2].

Protocol (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

  • Animal Models: SOD1-G93A mice
  • Dosages: 30 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 315.37
Formula

C19H17N5

CAS No. 1125758-85-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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