BKCa activator-1

BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model[1].

Product Specifications

UNSPSC

12352005

Target

Potassium Channel

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Others

Smiles

OC1=C(C=CC(NCCCCCN2CCOCC2)=C1)OC3=C(C(F)=C(C(F)=C3F)C(F)(F)F)F

Molecular Formula

C22H23F7N2O3

Molecular Weight

496.42

References & Citations

[1]Park SB, et al., Discovery of Diphenyl Ether Derivatives as Novel BKCa Channel Activators: Structure-Activity Relationship, Cryo-EM Complex Structures, and In Vivo Animal Studies. J Med Chem. 2025 Feb 27;68 (4) :4259-4286.