CFTRinh-172
Catalog No.S7139 Synonyms: CFTR inhibitor 172
Molecular Weight(MW): 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.
3 Customer Reviews
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CFTR inhibitor CFTR_inh172 leads to PGCs disorder in early zebrafish embryo. Analysis of localization of nanos1/vasa positive cells in embryos by WISH at 50% Epiboly stage with top view.
Reproduction, 2018, 156(3):261-268. CFTRinh-172 purchased from Selleck.
CFTR attenuated ox-LDL-induced NF-
Biosci Rep, 2017, 37(4). CFTRinh-172 purchased from Selleck.
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(A) K562 and SUP-B15 cells treated with 120 M and 90 M CFTRinh-172 respectivelyfor 48 h exhibited decreased CFTR and HDAC2 protein levels compared with the control.
Leuk Res, 2017, 57:9-19. CFTRinh-172 purchased from Selleck.
Purity & Quality Control
Choose Selective CFTR Inhibitors
Biological Activity
| Description | 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. | ||||||||||||||||
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| 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] |
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| Cell Data |
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| 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
| Kinase Assay: |
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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–. |
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Solubility (25°C)
| In vitro | DMSO | 82 mg/mL (200.29 mM) |
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| Water | Insoluble | |
| Ethanol | 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.
Chemical Information
| Molecular Weight | 409.4 |
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| Formula | C18H10F3NO3S2 |
| CAS No. | 307510-92-5 |
| Storage | powder |
| in solvent | |
| Synonyms | CFTR inhibitor 172 |
Bio Calculators
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Molarity Calculator
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.
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