CFTRinh-172

Catalog No.S7139 Batch:S713901

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Technical Data

Formula

C18H10F3NO3S2
Molecular Weight 409.4 CAS No. 307510-92-5
Solubility (25°C)* In vitro DMSO 82 mg/mL (200.29 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[4]
  • Animal Models

    An adult mouse model of Vibrio cholerae-induced diarrhea

  • Dosages

    20 µg/6 h

  • Administration

    Intraperitoneal administration

Customer Product Validation

Data from [Data independently produced by , , Reproduction, 2018, 156(3):261-268]

Data from [Data independently produced by , , Biosci Rep, 2017, 37(4)]

Data from [Data independently produced by , , Leuk Res, 2017, 57:9-19]

Selleck's CFTRinh-172 has been cited by 33 publications

Efferocytosis reprograms the tumor microenvironment to promote pancreatic cancer liver metastasis [ Nat Cancer, 2024, 10.1038/s43018-024-00731-2] PubMed: 38355776
Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells [ Cell Rep, 2023, 42(5):112529] PubMed: 37200193
UBE3C Facilitates the ER-Associated and Peripheral Degradation of Misfolded CFTR [ Cells, 2023, 12(23)2741] PubMed: 38067172
The synthetic aminoglycoside ELX-02 induces readthrough of G550X-CFTR producing superfunctional protein that can be further enhanced by CFTR modulators [ Am J Physiol Lung Cell Mol Physiol, 2023, 324(6):L756-L770] PubMed: 37014818
CFTR mRNAs with nonsense codons are degraded by the SMG6-mediated endonucleolytic decay pathway [ Nat Commun, 2022, 13(1):2344] PubMed: 35487895
Downstream Alternate Start Site Allows N-Terminal Nonsense Variants to Escape NMD and Results in Functional Recovery by Readthrough and Modulator Combination [ J Pers Med, 2022, 12-91448] PubMed: 36143233
High cystic fibrosis transmembrane conductance regulator expression in childhood B-cell acute lymphoblastic leukemia acts as a potential therapeutic target [ Transl Cancer Res, 2022, 11(3):436-443] PubMed: 35402186
Utilisation of CFTR orthologues to evaluate new therapies for cystic fibrosis [ University of Bristol, 2022, ] PubMed: None
A deep learning approach to identify gene targets of a therapeutic for human splicing disorders [ Nat Commun, 2021, 12(1):3332] PubMed: 34099697
Anti-Inflammatory and Anti-Oxidant Effect of Dimethyl Fumarate in Cystic Fibrosis Bronchial Epithelial Cells [ Cells, 2021, 10(8)2132] PubMed: 34440900

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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