CFTR (inh)-172 is an reversibly inhibitor ofCFTR short-circuit current in less than 2 minutes in a voltage-independent manner with Ki ~300 nM.
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The cystic fibrosis transmembrane conductance regulator (CFTR) protein is cAMP-activated epithelial Cl- channel required for fluid secretion in the intestine and airways. CFTR(inh)-172 reversibly inhibited CFTR short-circuit current in a voltage-independent manner with a KI of approximately 300nM. CFTR(inh)-172 significantly inhibited CFTR at dosages of 0.3-0.6μM. In CFTR-expressing FRT cells, treatment with CFTR(inh)-172 led to a dose-dependent inhibition of short-circuit current with a Kd value of approximately 300nM. CFTR(inh)-172 at 5μM did not block Ca2+-activated Cl- secretion in polarized human bronchial epithelial cell or volume-activated Cl- currents in FRT cells. A single intraperitoneal injection of CFTR(inh)-172 (250μg/kg) in mice before cholera toxin infusion prevented fluid accumulation in the toxin-treated intestinal loops[3].
作用机制
CFTR(inh)-172 is a potent blocker of the CFTR Cl- channel that reversibly inhibits CFTR short-circuit current[3].
CFTR(inh)-172 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
rat FRT cells
Function assay
Inhibition of human wild type CFTR expressed in rat FRT cells assessed as chloride current by short-circuit current measurements, IC50=0.38 μM
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