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A 438079 hydrochloride

Catalog No. T2673 CAS 899431-18-6

Synonyms: A 438079 (hydrochloride), A-438079 hydrochloride, A-438079 HCl

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

A 438079 hydrochloride Chemical Structure

A 438079 hydrochloride, CAS 899431-18-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 66.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 189.00
50 mg	In stock	$ 312.00
100 mg	In stock	$ 547.00
1 mL * 10 mM (in DMSO)	In stock	$ 116.00

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Purity: 99.74%

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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 hydrochloride, A-438079 HCl
Molecular Weight	342.61
Formula	C13H10Cl3N5
CAS No.	899431-18-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 1.7 mg/mL (5 mM)), Heating is recommended.

DMSO: 34.3 mg/mL (100 mM)

References and Literature

1. McGaraughty S, et al. Neuroscience. 2007, 146(4), 1817-1828. 2. Mesuret G, et al. CNS Neurosci Ther. 2014, 20(6), 556-564. 3. Marcellino D, et al. J Neural Transm. 2010, 17(6), 681-687. 4. Martins JP, et al. Br J Pharmacol. 2012, 165(1), 183-196. 5. Su Q, Tian Y, Liu Z, et al. Purinergic P2X7 receptor blockade mitigates alcohol-induced steatohepatitis and intestinal injury by regulating MEK1/2-ERK1/2 signaling and egr-1 activity[J]. International immunopharmacology. 2019 Jan;66:52-61.

Citations

1. Wang J, Han Y, Wang M, et al. The inhibitory effect of Yam polysaccharides on acrylamide‐induced programmed cell death in RAW 264.7 cells. Food Science & Nutrition. 2022 2. Su Q, Tian Y, Liu Z, et al. Purinergic P2X7 receptor blockade mitigates alcohol-induced steatohepatitis and intestinal injury by regulating MEK1/2-ERK1/2 signaling and egr-1 activity. International Immunopharmacology. 2019 Jan;66:52-61 3. Zhang A, Jin D, Han Y, et al.The effects of Yam polysaccharides on acrylamide-induced RAW264. 7 cell polarization.Journal of Food Bioactives.2023, 23.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library Ion Channel Inhibitor Library Bioactive Compound Library

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Keywords

A 438079 hydrochloride 899431-18-6 Membrane transporter/Ion channel Neuroscience P2X Receptor A 438079 P2XRs A438079 A438079 Hydrochloride A 438079 (hydrochloride) Inhibitor A 438079 Hydrochloride inhibit A-438079 Hydrochloride A-438079 hydrochloride A-438079 HCl A-438079 inhibitor

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