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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 90 In-stock
25 mg USD 190 In-stock
50 mg USD 330 In-stock
100 mg USD 530 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

A-804598 Related Antibodies

Top Publications Citing Use of Products

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P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

P2X7 Receptor

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-804598 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](/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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (101.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1709 mL 15.8544 mL 31.7088 mL 79.2720 mL
5 mM 0.6342 mL 3.1709 mL 6.3418 mL 15.8544 mL
10 mM 0.3171 mL 1.5854 mL 3.1709 mL 7.9272 mL
15 mM 0.2114 mL 1.0570 mL 2.1139 mL 5.2848 mL
20 mM 0.1585 mL 0.7927 mL 1.5854 mL 3.9636 mL
25 mM 0.1268 mL 0.6342 mL 1.2684 mL 3.1709 mL
30 mM 0.1057 mL 0.5285 mL 1.0570 mL 2.6424 mL
40 mM 0.0793 mL 0.3964 mL 0.7927 mL 1.9818 mL
50 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5854 mL
60 mM 0.0528 mL 0.2642 mL 0.5285 mL 1.3212 mL
80 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9909 mL
100 mM 0.0317 mL 0.1585 mL 0.3171 mL 0.7927 mL
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A-804598 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-8045981125758-85-1A804598A 804598P2X ReceptorP2XRsInhibitorinhibitorinhibit

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