A-804598

For research use only.

Catalog No.S8725

1 publication

A-804598 Chemical Structure

Molecular Weight(MW): 315.37

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.

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Selleck's A-804598 has been cited by 1 publication

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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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: SOD1-G93A mice
  • Dosages: 30 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (199.76 mM)
Ethanol 6 mg/mL (19.02 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 315.37
Formula

C19H17N5

CAS No. 1125758-85-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(C1=CC=CC=C1)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID