DC Chemicals Supply: PPQ-102, Cas: 931706-15-9 ,Cat No. DC7483, Purity>98%, In stock.
Contact: website: www.dcchemicals.com,
sales@dcchemicals.com,order@dcchemicals.com,info@dcchemicals.com,
Tel: +86-21-58447131;Fax:+86-21-61642470；
PPQ-102|cas 931706-15-9, Synonym name: CFTR Inhibitor; PPQ102; PPQ 102, Chemical name: , Molecule weight: 438.48, Molecule Formula: C26H22N4O3
PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC 50approximately 90 nM.
PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC 50approximately 90 nM.
IC50 value: 90 nM [1]
Target: CFTR
in 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].
没有评论:
发表评论