IK1 inhibitor PA-6

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].

Product Specifications

CAS Number

[500715-03-7]

Product Name Alternative

PA-6

UNSPSC

12352005

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/ik1-inhibitor-pa-6.html

Purity

99.29

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

N=C(C1=CC=CC=C1)NC2=CC=C(OCCCCCOC3=CC=C(NC(C4=CC=CC=C4)=N)C=C3)C=C2

Molecular Formula

C31H32N4O2

Molecular Weight

492.61

References & Citations

[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.