CAS:931706-15-9PPQ-102

Synonyms: CFTR Inhibitor

PPQ-102 is a potent and voltage-independent CFTR inhibitor, which completely inhibit CFTR chloride current with IC50 approximately 90 nM.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

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实验数据

技术信息

CAS号

931706-15-9

储存条件

分子式

C26H22N4O3

运输

蓝冰

分子量

438.48

别名

CFTR Inhibitor

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

生物活性

描述CFTR is a chloride channel, that controls ion and water secretion and absorption in epithelial tissues. CFTR protein dysfunction leads to abnormal ion transport across the airway epithelium^[3]. PPQ2 as a small molecule CFTR inhibitor that completely inhibited CFRR chloride current with IC50 value of 90 nM^[4]. In vitro, PPQ-102 at the dose of 10µM inhibited CFTR almost 100% in (nonpermeabilized) human intestinal (T84) and bronchial cells following maximal CFTR activation by forskolin and IBMX. However, PPQ-102 did not inhibit calcium-activated chloride channels or cellular cAMP production^[4]. PPQ-102 also inhibited the volume-regulated anion channel (VRAC) conductance with IC50 value of 20μM in HEK293 cells^[5]. Treatment of NCI-H292 cells with 10μM PPQ-102 induced a two-fold increase in VEGF-A synthesis^[3]. In the presence of NADPH, PPQ-102 lost in hepatic microsomes about 60% within 30min. No loss of PPQ-102 was seen in the absence of NADPH. In vivo, PPQ-102 was undetectable in serum, kidney and urine at 30-60 min after intravenous administration of 300μg PPQ-102 by LC/MS assay with sensitivity better than 100nM^[6].
作用机制PPQ-102 inhibits CFTR by an altered channel gating mechanism, with stabilization of the channel closed state^[4].