A 804598

Modify Date: 2024-01-04 13:39:26

A 804598 Structure
A 804598 structure
Common Name A 804598
CAS Number 1125758-85-1 Molecular Weight 315.37200
Density N/A Boiling Point N/A
Molecular Formula C19H17N5 Melting Point N/A
MSDS Chinese Flash Point N/A
Symbol GHS06
GHS06
Signal Word Danger

 Use of A 804598


A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay. [1]In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. [2]

 Names

Name 2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine
Synonym More Synonyms

 A 804598 Biological Activity

Description A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay. [1]In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. [2]
Related Catalog
References

[1]. Donnelly-Roberts DL et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009 Jan, 56(1):223-9.

[2]. Able SL et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br J Pharmacol, 2011 Jan, 162(2):405-14.

 Chemical & Physical Properties

Molecular Formula C19H17N5
Molecular Weight 315.37200
Exact Mass 315.14800
PSA 73.10000
LogP 4.29848
Storage condition -20℃

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
RIDADR UN 2811 6.1 / PGIII

 Synonyms

N-Cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
A 804598
A-804598