Drug intelligence / Profile preview

BL1249

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous
01

Overview

BL1249 is a small molecule potassium channel opener that acts as a selective agonist for the two-pore domain potassium (K2P) channels, specifically TREK-1 (KCNK2) and TREK-2 (KCNK10). Originally identified by Bristol-Myers Squibb as a bladder-selective potassium channel opener, it has become a widely used research tool for investigating the physiological roles of TREK channels. In the context of respiratory research, BL1249 has demonstrated anti-inflammatory potential by repolarizing the plasma membrane of alveolar epithelial cells, which are often depolarized during bacterial (e.g., *Pseudomonas aeruginosa*) or viral (e.g., Influenza-A) infections. This repolarization leads to a reduction in the production of reactive oxygen species (ROS) and the secretion of pro-inflammatory cytokines such as CXCL10, CCL2, and IL-6, suggesting a potential therapeutic role in mitigating lung injury and inflammation.

Other names
(5,6,7,8-tetrahydronaphthalen-1-yl)-[2-(1H-tetrazol-5-yl)phenyl]amine
02

Targets

KCNK10KCNK4 (Potassium channel subfamily K member 4)KCNK2 (Potassium channel subfamily K member 2)

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