500715-03-7

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].

PA-6 (Pentamidine-Analogue 6) is a selective and potent IK1 (inward rectifier potassium current) inhibitor th at terminates atrial fibrillation and does not cause ventricular arrhythmias in go at and dog models. PA-6 interacts with the cytoplasmic pore region of the KIR2.1 (KCNJ2) ion channel.

[1] Takanari H, et al. Efficient and specific cardiac IK? inhibition by a new pentamidine analogue. Cardiovasc Res. 2013 Jul 1;99(1):203-14. DOI:10.1093/cvr/cvt103
[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. DOI:10.1111/bph.13869
[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. DOI:10.1186/s12929-017-0352-x