Drug intelligence / Profile preview

A740003

Development stage
Preclinical
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

A740003 is a potent, selective, and competitive small molecule antagonist of the P2X7 receptor, an ATP-gated ion channel. Developed by Abbott Laboratories, it is primarily used as a pharmacological tool to investigate the role of P2X7 signaling in inflammatory and nociceptive processes. The P2X7 receptor plays a critical role in the activation of the NLRP3 inflammasome, leading to the maturation and release of pro-inflammatory cytokines such as interleukin-1β (IL-1β). Research indicates that A740003 can reduce inflammasome activation and cytokine release in various models, including breast cancer cell lines where it inhibits neutrophil extracellular trap (NET)-induced tumor progression. While it has shown efficacy in preclinical models of chronic pain and inflammation, it is predominantly recognized as a high-affinity reference compound in purinergic signaling research.

Other names
N-[1-[[(Cyanoamino)(methylamino)methylene]amino]-2,2-dimethylpropyl]-2-(4-methylphenyl)acetamide
02

Targets

P2RX7 (P2X purinoceptor 7)

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