A selective P2X7 antagonist (IC50s = 40 and 18 nM for human and rat receptors

A-740003 – 1 mg

Brand:
Cayman
CAS:
861393-28-4
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).{33388} It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).{33388} It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.{33388} A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.{22913,33386,33387}  

 

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Description

A selective P2X7 antagonist (IC50s = 40 and 18 nM for human and rat receptors, respectively); blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively); effective in vivo when administered intraperitoneally

Formal name: N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy-benzeneacetamide

Synonyms: 

Molecular weight: 474.6

CAS: 861393-28-4

Purity: ≥98%

Formulation: A crystalline solid

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

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