A 438079 hydrochloride

Name: A 438079 hydrochloride
Brand: MedChemExpress
SKU: HY-15488A
Rating: 5.0 (14 reviews)

Cat. No.: HY-15488A Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

A 438079 (hydrochloride) is a potent, and selective P2X₇ receptor antagonist with pIC₅₀ of 6.9.

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

A 438079 hydrochloride Chemical Structure

CAS No. : 899431-18-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 83	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of A 438079 hydrochloride:

A 438079 In-stock

12 Publications Citing Use of MCE A 438079 hydrochloride

IHC

: A 438079 hydrochloride purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401. [Abstract]; Western analysis of protein expression levels in the treatment of compounds such as A 438079.

: A 438079 hydrochloride purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401. [Abstract]; Immunohistochemistry staining analysis of effects of rHSP90 and A438079 on neurobehavior and neurogenesis 48 h after SAH.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

A 438079 (hydrochloride) is a potent, and selective P2X₇ receptor antagonist with pIC₅₀ of 6.9.

IC₅₀ & Target

P2X7 Receptor

In Vitro

In 1321N1 cells stably expressing rat P2X₇?receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC₅₀ of 321 nM. A 438079 is also selective for the P2X₇ receptor, at concentrations up to 100 μM^[1].

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

In Vivo

A 438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A 438079 (100 and 300 μmol/kg, i.p.) signi?cantly raises withdrawal thresh-olds in both the SNL and CCI models^[1].
Intraperitoneal injection of A 438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus. A 438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25 mg/kg)^[2].
?A 438079 partially but signi?cantly prevents the 6-OHDA-induced depletion of striatal DA stores^[3].
Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model^[4].

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

Molecular Weight

342.61

Formula

C₁₃H₁₀Cl₃N₅

CAS No.

899431-18-6

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (291.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.92 mM; ultrasonic and warming and heat to 80°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9188 mL	14.5939 mL	29.1877 mL
5 mM	0.5838 mL	2.9188 mL	5.8375 mL
10 mM	0.2919 mL	1.4594 mL	2.9188 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (7.30 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 (7.30 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 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 (7.30 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).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

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: 99.92%

Select Batch:

Data Sheet (284 KB) SDS (544 KB)

COA (253 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28. [Content Brief]

[2]. Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64. [Content Brief]

[3]. Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7. [Content Brief]

[4]. Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96. [Content Brief]

Kinase Assay ^[1]	Human astrocytoma cells, 1321N1, are grown to stably express rat P2X₇, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1 and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca²⁺ concentrations are assessed in all of the cell lines using the Ca²⁺ chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca²⁺ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10^-10 to 10^-4 M. BzATP or ATP concentrations corresponds to the EC₇₀ values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and ﬂuorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC₅₀ or pIC₅₀ values are derived from a single curve ﬁt. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	To confirm A 438079 reach the brain after systemic administration, P10 rat pups are injected with 5 mg/kg A 438079 and killed either 10 min, 30 min, or 2 h later (n=4 per group). Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma. Samples are analyzed using liquid chromatography-mass spectrometry (LC-MS/MS) by a service provider. Briefly, protein is precipitated from 50 μL aliquots of the individual plasma or brain tissue homogenate, and A 438079 is quantified by LC-MS/MS from a five-point standard curve. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28. [Content Brief] [2]. Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64. [Content Brief] [3]. Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7. [Content Brief] [4]. Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.9188 mL	14.5939 mL	29.1877 mL	72.9693 mL
DMSO	5 mM	0.5838 mL	2.9188 mL	5.8375 mL	14.5939 mL
	10 mM	0.2919 mL	1.4594 mL	2.9188 mL	7.2969 mL
	15 mM	0.1946 mL	0.9729 mL	1.9458 mL	4.8646 mL
	20 mM	0.1459 mL	0.7297 mL	1.4594 mL	3.6485 mL
	25 mM	0.1168 mL	0.5838 mL	1.1675 mL	2.9188 mL
	30 mM	0.0973 mL	0.4865 mL	0.9729 mL	2.4323 mL
	40 mM	0.0730 mL	0.3648 mL	0.7297 mL	1.8242 mL
	50 mM	0.0584 mL	0.2919 mL	0.5838 mL	1.4594 mL
	60 mM	0.0486 mL	0.2432 mL	0.4865 mL	1.2162 mL
	80 mM	0.0365 mL	0.1824 mL	0.3648 mL	0.9121 mL
	100 mM	0.0292 mL	0.1459 mL	0.2919 mL	0.7297 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.