A-804598

Name: A-804598
Brand: MedChemExpress
SKU: HY-100483
Rating: 5.0 (3 reviews)

Cat. No.: HY-100483 Purity: 98.55%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 30	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE A-804598

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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

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	15 nM Compound: 6; A-804598	Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader	[PMID: 33822617]

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.

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.

1125758-85-1

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
10 mM	0.3171 mL	1.5854 mL	3.1709 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 98.55%

Select Batch:

Data Sheet (279 KB) SDS (419 KB)

COA (254 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Donnelly-Roberts DL et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009 Jan, 56(1):223-9. [Content Brief]

[2]. Yingbo He et al. The role of microglial P2X7: modulation of cell death and cytokine release. Neuroinflammation, 2017 Jul, 14(1):135. [Content Brief]

[3]. Paola Fabbrizio et al. P2X7 Receptor Activation Modulates Autophagy in SOD1-G93A Mouse Microglia.Cell Neurosci, 2017 Aug, 11:249. [Content Brief]

Complete Stock Solution Preparation Table

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

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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A-804598

Customer Review

A-804598 Related Antibodies

3 Publications Citing Use of MCE A-804598

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All P2X Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

A-804598 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

A-804598 Related Classifications

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