CFTRinh-172 307510-92-5

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Molecular Weight:

409.4 CFTRinh-172 is a voltage-independent, Selective CFTR Inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.

Biological Activity

CFTRinh-172 dose- and time-dependently inhibits CFTR-mediated I- transportation, and effectively inhibits CFTR activation by multiple types of agonists or activators. CFTRinh-172, as a selective CFTR channel inhibitor, also completely abolishes the Cl− current in the rabbit acinar and duct cells of rabbit lacrimal gland. CFTRinh-172 also induces ROS production, mitochondrial failure, and
activation of the NF-κB signaling pathway, independently of CFTR
inhibition.


CFTRinh-172 (20 µg/6 h) completely abolishes the V. cholerae-induced
intestinal fluid secretion without affecting V. cholerae growth in vivo.






Screening procedures


Assays are done using a customized screening system consisting of a 3-meter robotic arm, CO2 incubator, plate washer, liquid-handling workstation, bar code reader,
delidding station, and two FLUOstar fluorescence platereaders, each
equipped with two syringe pumps and HQ500/20X (500 ± 10 nm) excitation
and HQ535/30M (535 ± 15 nm) emission filters.


The robotic system is
integrated using SAMI version 3.3 software modified for two
platereaders. Custom software is written in Microsoft VBA (Visual Basic
for Applications) to compute base-line–subtracted, normalized
fluorescence slopes (giving halide influx rates) from stored data files.
The assay is set up by loading the incubator (37°C, 90% humidity, 5% CO2)
with 40–60 96-well plates containing the FRT cells, and loading a
carousel with 96-well plates containing test compounds and disposable
plastic pipette tips.


To initiate the assay, each well of a 96-well
plate is washed three times in PBS (300 μl/wash), leaving 50 μL PBS. Ten
microliters of a CFTR-activating cocktail (5 μM forskolin, 100 μM IBMX,
25 μM apigenin in PBS) is added, and after 5 minutes one test compound
(0.5 μL of 1 mM DMSO solution) is added to each well to give 10 μM final
concentration. After 10 minutes, 96-well plates are transferred to a
platereader for fluorescence assay.


Each well is assayed individually
for CFTR-mediated I– transport by recording fluorescence continuously
(200 ms per point) for 2 seconds (base line) and then for 12 seconds
after rapid

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Product Categories : Transmembrane Transporters > CFTR Inhibitor