Home Transmembrane Transporters CFTR inhibitor CFTRinh-172 For research use only.

CFTRinh-172

Synonyms: CFTR inhibitor 172

CFTRinh-172 (CFTR inhibitor 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.

CFTRinh-172 Chemical Structure

CFTRinh-172 Chemical Structure

CAS No. 307510-92-5

Purity & Quality Control

CFTRinh-172 Related Products

Signaling Pathway

CFTR Signaling Pathways

CFTR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 18691893
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Biological Activity

Description CFTRinh-172 (CFTR inhibitor 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.
Targets
CFTR [1]
(in human airway cells)
300 nM(Ki)
In vitro
In vitro CFTRinh-172 dose- and time-dependently inhibits CFTR-mediated I- transportation, and effectively inhibits CFTR activation by multiple types of agonists or activators. [1] 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. [2] CFTRinh-172 also induces ROS production, mitochondrial failure, and activation of the NF-κB signaling pathway, independently of CFTR inhibition. [3]
Kinase Assay 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 (<0.5 seconds) addition of 165 μL of isosmolar PBS in which 137 mM Cl– was replaced by I–.
Cell Research Cell lines Fischer rat thyroid (FRT) cells
Concentrations ~1 mM
Incubation Time 24 hours
Method

Cell toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor.
In Vivo
In vivo CFTRinh-172 (20 µg/6 h) completely abolishes the V. cholerae-induced intestinal fluid secretion without affecting V. cholerae growth in vivo. [4]
Animal Research Animal Models An adult mouse model of Vibrio cholerae-induced diarrhea
Dosages 20 µg/6 h
Administration Intraperitoneal administration

Chemical Information & Solubility

Molecular Weight 409.4 Formula

C18H10F3NO3S2
CAS No. 307510-92-5 SDF Download CFTRinh-172 SDF
Smiles C1=CC(=CC(=C1)N2C(=O)C(=CC3=CC=C(C=C3)C(=O)O)SC2=S)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (200.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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