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PPQ-102
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PPQ-102图片
CAS NO:931706-15-9
包装:1mg
市场价:1155元

产品介绍
PPQ-102 (CFTR Inhibitor) 是一种可逆的 CFTR 抑制剂,可完全抑制 CFTR 氯化物电流 (IC50 ~90 nM)。
Cas No.931706-15-9
别名CFTR Inhibitor
化学名7,9-dimethyl-6-(5-methylfuran-2-yl)-11-phenyl-5,6-dihydropyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(7H,9H)-dione
Canonical SMILESCC(O1)=CC=C1C(NC2=CC=CC=C2N34)C4=C(N(C5=O)C)C(C(N5C)=O)=C3C6=CC=CC=C6
分子式C26H22N4O3
分子量438.48
溶解度DMF: 0.2 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[1]. Tradtrantip L, et al. Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model. J Med Chem. 2009 Oct 22;52(20):6447-55.
[2]. Stewart AK, et al. SLC26 anion exchangers of guinea pig pancreatic duct: molecular cloning and functional characterization. Am J Physiol Cell Physiol. 2011 Aug;301(2):C289-303.
[3]. Martin C, et al. CFTR dysfunction induces vascular endothelial growth factor synthesis in airway epithelium. Eur Respir J. 2013 Dec;42(6):1553-62.