1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. A-804598

A-804598 

Cat. No.: HY-100483 Purity: 98.83%
Handling Instructions

A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.

For research use only. We do not sell to patients.

A-804598 Chemical Structure

A-804598 Chemical Structure

CAS No. : 1125758-85-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
25 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 696 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively[1].

IC50 & Target

IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor)[1]

In Vitro

Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity[2].

Cell Cytotoxicity Assay[2]

Cell Line: microglial cell
Concentration: 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 1 hour
Result: Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia.
In Vivo

A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease[3].

Animal Model: Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice [3]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; five times a week
Result: Decreased SQSTM1/p62 expression.
Molecular Weight

315.37

Formula

C₁₉H₁₇N₅

CAS No.

1125758-85-1

SMILES

C[[email protected]](/N=C(NC1=C2C=CC=NC2=CC=C1)/NC#N)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (101.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1709 mL 15.8544 mL 31.7088 mL
5 mM 0.6342 mL 3.1709 mL 6.3418 mL
10 mM 0.3171 mL 1.5854 mL 3.1709 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.93 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
A-804598
Cat. No.:
HY-100483
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