IK1 inhibitor PA-6 (PA-6) 是一种喷他脒类似物，是有效的、选择性的 IK1 (KIR2.x离子通道携带向内整流电流) 抑制剂，人和老鼠中对KIR2.x 电流的 IC50 值为 12-15 nM。IK1 inhibitor PA-6 (PA-6) 可上调 KIR2.1 的蛋白表达，诱导细胞内KIR2.1 的蛋白的积累。IK1 inhibitor PA-6 (PA-6) 有治疗房颤和心律失常的潜力。
| Cas No. | 500715-03-7 |
| 别名 | PA-6 |
| Canonical SMILES | N=C(C1=CC=CC=C1)NC2=CC=C(OCCCCCOC3=CC=C(NC(C4=CC=CC=C4)=N)C=C3)C=C2 |
| 分子式 | C31H32N4O2 |
| 分子量 | 492.61 |
| 溶解度 | DMSO: 125 mg/mL (253.75 mM) |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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]. [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.
[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. |
