| 常用名 | PPQ-102 | CAS号 | 931706-15-9 |
|---|---|---|---|
| 价格 | ¥需询单/1kg ¥需询单/1g ¥需询单/1mg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情(用途,包装等)
用途: PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC50 of ~90 nM. IC50 value: 90 nM [1]Target: CFTRin vitro: The most potent compound, 7,9-dimethyl-11-phenyl-6-(5-methylfuran-2-yl)-5,6-dihydro-pyrimido[4',5'-3,4]pyrrolo[1,2-a]quinoxaline-8,10-(7H,9H)-dione, PPQ-102, completely inhibited CFTR chloride current with IC(50) approximately 90 nM. The PPQs, unlike prior CFTR inhibitors, are uncharged at physiological pH, and therefore not subject to membrane potential-dependent cellular partitioning or block efficiency. Patch-clamp analysis confirmed voltage-independent CFTR inhibition by PPQ-102 and showed stabilization of the channel closed state [1]. The three gpSlc26 anion transporters exhibited distinct pharmacological profiles of (36)Cl(-) influx, including partial sensitivity to CFTR inhibitors Inh-172 and GlyH101, but only Slc26a11 was inhibited by PPQ-102 [2]. Airway epithelial NCI-H292 cells and primary cultures of noncystic fibrosis human airway epithelial cells were treated with cystic fibrosis transmembrane conductance regulator (CFTR) inhibitors (CFTR-inh(172) or PPQ-102) or transfected with a CFTR small interfering (si)RNA with or without a selective epidermal growth factor receptor tyrosine kinase inhibitor [3].in vivo: PPQ-102 prevented cyst expansion and reduced the size of preformed cysts in a neonatal kidney organ culture model of polycystic kidney disease. PPQ-102 is the most potent CFTR inhibitor identified to date [1]. 物理化学性质: CAS号:931706-15-9 常用中文名:PPQ-102 常用英文名:PPQ 102 分子式:C26H22N4O3 分子量:438.478 密度:1.4±0.1 g/cm3 沸点:648.7±65.0 °C at 760 mmHg 熔点:N/A 闪点:346.1±34.3 °C 储存条件:-20℃ |