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IK1 inhibitor PA-6

Names

[ CAS No. ]:
500715-03-7

[ Name ]:
IK1 inhibitor PA-6

Biological Activity

[Description]:

IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 12-15 nM (KIR2.x currents)[1].


[References]

[1]. Takanari H, et al. Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue. Cardiovasc Res. 2013 Jul 1;99(1):203-14.

[2]. Ji Y, et al. The inward rectifier current inhibitor PA-6 terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. Br J Pharmacol. 2017 Aug;174(15):2576-2590.

[3]. Ji Y, et al. PA-6 inhibits inward rectifier currents carried by V93I and D172N gain-of-function KIR2.1 channels, but increases channel protein expression. J Biomed Sci. 2017 Jul 15;24(1):44.

Chemical & Physical Properties

[ Molecular Formula ]:
C31H32N4O2

[ Molecular Weight ]:
492.61


Related Compounds

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