A-438079 Hydrochloride P2 Receptor antagonist | CAS 899431-18-6

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other P2 Receptor Inhibitors	A-804598 MRS 2578 A-740003 5-BDBD Gefapixant AF-353 A-317491 Minodronic acid Diquafosol Tetrasodium BX430

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
HEK293 cells	Function assay	Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay, IC50=0.12303 μM
human 1321N1 cells	Function assay	Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR, IC50=0.12589 μM
human THP1 cells	Function assay	Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake, IC50=0.12589 μM
HEK cells	Function assay	Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake, IC50=0.31623 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	342.61	Formula	C₁₃H₁₀Cl₃N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	899431-18-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=C(C(=C1)Cl)Cl)C2=NN=NN2CC3=CN=CC=C3.Cl

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (198.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 68 mg/mL

Water : 10 mg/mL (超声加热十分钟)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (87.56mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	P2X7 (in 1321N1 cells) 6.9(pIC50)
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.
In vivo	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 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A-438079 reduces nociceptive behaviour scores in the HC model. 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.) significantly raises withdrawal thresholds in both the SNL and CCI models.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17478048/ [2] https://pubmed.ncbi.nlm.nih.gov/24750893/ [3] https://pubmed.ncbi.nlm.nih.gov/20387084/ [4] https://pubmed.ncbi.nlm.nih.gov/21675966/

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A-438079 Hydrochloride P2X Receptor Antagonist

Chemical Structure

Molecular Weight: 342.61