A potent and selective competitive antagonist of the P2X7 receptor (IC50s = 9.9 and 10.9 nM in 132N1 cells transfected with the rat or mouse receptor

A-804598 – 10 mg

Brand:
Cayman
CAS:
1125758-85-1
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

A-804598 is a potent and selective competitive antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel, with IC50 values of 9.9 and 10.9 nM in 132N1 cells transfected with the rat or mouse receptor, respectively.{38237} It inhibits IL-1β release in human THP-1 cells stimulated with LPS and IFN-γ (IC50 = 8.5 nM). A-804598 is selective for P2X7 receptors over other P2X and P2Y receptors at concentrations up to 100 µM and over many G protein-coupled receptors, enzymes, transporters, and ion channels. A-804598 (25 mg/kg) prevents footshock-induced increases in IL-1β mRNA in the paraventricular nucleus of the rat hypothalamus.{38236}  

 

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Description

A potent and selective competitive antagonist of the P2X7 receptor (IC50s = 9.9 and 10.9 nM in 132N1 cells transfected with the rat or mouse receptor, respectively), inhibits IL-1β release in LPS and IFN-γ-stimulated THP-1 cells (IC50 = 8.5 nM); selective over other P2X and P2Y receptors at concentrations up to 100 µM; prevents footshock-induced increases in IL-1β mRNA in the rat hypothalamus ,

Formal name: N-cyano-N”-[(1S)-1-phenylethyl]-N’-5-quinolinyl-guanidine

Synonyms: 

Molecular weight: 315.4

CAS: 1125758-85-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience

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