BL-1249

BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) [1][2].

Product Specifications

CAS Number

[18200-13-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/bl-1249.html

Purity

99.81

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C1(NC2=C3CCCCC3=CC=C2)=CC=CC=C1C4=NN=NN4

Molecular Formula

C17H17N5

Molecular Weight

291.35

Precautions

H302, H315, H319, H335

References & Citations

[1]Tertyshnikova S, et al. BL-1249 [ (5,6,7,8-tetrahydro-naphthalen-1-yl) -[2- (1H-tetrazol-5-yl) -phenyl]-amine]: a putative potassium channel opener with bladder-relaxant properties. J Pharmacol Exp Ther. 2005 Apr;313 (1) :250-9.|[2]Pope L, et al. Protein and Chemical Determinants of BL-1249 Action and Selectivity for K2P Channels. ACS Chem Neurosci. 2018 Dec 19;9 (12) :3153-3165.|[3]Iwaki Y, et al. Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249. Bioorg Med Chem Lett. 2019 Jul 1;29 (13) :1601-1604.