A-804598

Catalog No.S8725 Batch:S872501

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Technical Data

Formula

C19H17N5
Molecular Weight 315.37 CAS No. 1125758-85-1
Solubility (25°C)* In vitro DMSO 63 mg/mL (199.76 mM)
Ethanol 6 mg/mL (19.02 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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 Study:

[2]
  • Animal Models

    SOD1-G93A mice

  • Dosages

    30 mg/kg

  • Administration

    i.p.

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

Apelin-13/APJ induces cardiomyocyte hypertrophy by activating the Pannexin-1/P2X7 axis and FAM134B-dependent reticulophagy [ J Cell Physiol, 2022, 10.1002/jcp.30685] PubMed: 35128666
Activation of the purinergic receptor P2X7 improves hepatosteatosis by promoting lipophagy [ FEBS Lett, 2021, 10.1002/1873-3468.14207] PubMed: 34652813
Cathelicidin aggravates myocardial ischemia/reperfusion injury via activating TLR4 signaling and P2X7R/NLRP3 inflammasome. [ J Mol Cell Cardiol, 2020, 139:75-86] PubMed: 31982429

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.