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A-804598

Catalog No. T3639   CAS 1125758-85-1
Synonyms: A 804598

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

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A-804598 Chemical Structure
A-804598, CAS 1125758-85-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 39.00
5 mg In stock $ 63.00
10 mg In stock $ 85.00
25 mg In stock $ 183.00
50 mg In stock $ 323.00
100 mg In stock $ 522.00
500 mg In stock $ 1,170.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).
Targets&IC50 P2X7R (human):11 nM, P2X7R (rat):10 nM, P2X7R (rat):9 nM
In vitro A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1]
In vivo According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2]
Synonyms A 804598
Molecular Weight 315.37
Formula C19H17N5
CAS No. 1125758-85-1

Storage

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

Solubility Information

DMSO: 31.5 mg/mL(100 mM)

TargetMolReferences and Literature

1. Donnelly-Roberts DL, et al. Neuropharmacology. 2009 Jan;56(1):223-9. 2. Able SL, et al. Br J Pharmacol. 2011 Jan;162(2):405-14.

TargetMolCitations

1. Zhong T, Chen S, Deng K, et al.Magnesium alleviates extracellular histone-induced apoptosis and defective bacterial phagocytosis in macrophages by regulating intracellular calcium signal.International Immunopharmacology.2024, 132: 111870.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Membrane Protein-targeted Compound Library Bioactive Compound Library Ion Channel Inhibitor Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library CNS-Penetrant Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

A-804598 1125758-85-1 Membrane transporter/Ion channel Neuroscience P2X Receptor A804598 A 804598 P2XRs Inhibitor inhibit inhibitor

 

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