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A 438079 hydrochloride

Name: A 438079 hydrochloride
Brand: TargetMol
SKU: T2673
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2673Cas No. 899431-18-6

Alias A-438079 hydrochloride, A-438079 HCl, A 438079 (hydrochloride)

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

A 438079 hydrochloride

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Purity: 99.89%

Catalog No. T2673Alias A-438079 hydrochloride, A-438079 HCl, A 438079 (hydrochloride)Cas No. 899431-18-6

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

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$41	In Stock	In Stock
5 mg	$66	In Stock	In Stock
10 mg	$105	In Stock	In Stock
25 mg	$189	In Stock	In Stock
50 mg	$312	In Stock	In Stock
100 mg	$547	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$116	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.89%

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	A 438079 hydrochloride (A-438079 HCl) is a potent and selective P2X7 receptor antagonist with pIC50 of 6.9.
Targets&IC50	P2X7:6.9(pIC50)
In vitro	A-438079 has the capability to partially, yet significantly, inhibit the depletion of striatal dopamine (DA) levels induced by 6-OHDA. Pretreatment with A-438079 reduces the pain behavior index in the HC model. Intraperitoneal injection of A-438079 (5 and 15 mg/kg) 60 minutes post-epileptic seizure onset diminishes the severity of epileptic episodes and neuronal death within the hippocampus. Additionally, intravenous administration of 80 μMol/kg A-438079 in a neuropathic rat model significantly reduces both noxious and innocuous evoked activities in various categories of spinal neurons.
In vivo	A-438079 demonstrates selectivity towards the P2X7 receptor at concentrations of up to 100 μM. It effectively inhibits changes in intracellular calcium concentration induced by 10 μM BzATP in 1321N1 cells stably expressing the rat P2X7 receptor, with an IC50 of 321 nM.
Kinase Assay	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 ?uorescence 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 ?t.
Synonyms	A-438079 hydrochloride, A-438079 HCl, A 438079 (hydrochloride)

Chemical Properties

Molecular Weight	342.61
Formula	C₁₃H₁₀Cl₃N₅
Cas No.	899431-18-6
Smiles	Cl.Clc1cccc(-c2nnnn2Cc2cccnc2)c1Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 1.7 mg/mL (4.96 mM), Heating is recommended.

DMSO: 34.3 mg/mL (100.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.84 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9188 mL	14.5939 mL	29.1877 mL	145.9385 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.5838 mL	2.9188 mL	5.8375 mL	29.1877 mL
10 mM	0.2919 mL	1.4594 mL	2.9188 mL	14.5939 mL
20 mM	0.1459 mL	0.7297 mL	1.4594 mL	7.2969 mL
50 mM	0.0584 mL	0.2919 mL	0.5838 mL	2.9188 mL
100 mM	0.0292 mL	0.1459 mL	0.2919 mL	1.4594 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc