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CFTR(inh)-172

Catalog No. T2355 CAS 307510-92-5

Synonyms: CFTRinh 172, CFTR Inhibitor-172, CFTRinh-172, CFTRinh172

CFTR(inh)-172 (CFTR Inhibitor-172) is a voltage-independent, selective CFTR inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CFTR(inh)-172, CAS 307510-92-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 558.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.94%

Purity: 99.72%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	CFTR(inh)-172 (CFTR Inhibitor-172) is a voltage-independent, selective CFTR inhibitor.
Targets&IC50	CFTR:300 nM(Ki)
In vitro	Administering 20 μg of CFTRinh-172 over 6 hours fully abolished intestinal fluid secretion induced by Vibrio cholerae without affecting the growth of Vibrio cholerae within the body.
In vivo	CFTRinh-172, a selective inhibitor of the CFTR (Cystic Fibrosis Transmembrane Conductance Regulator) channel, effectively eliminates Cl- (chloride) currents in the lacrimal gland acinar and duct cells of rabbits. It exhibits time- and dose-dependent inhibition of CFTR-mediated iodide transport and efficiently inhibits the activation of CFTR by various agonists or activators. Notably, CFTRinh-172 induces the production of ROS (Reactive Oxygen Species), mitochondrial depletion, and the activation of the NF-κB (Nuclear Factor kappa-light-chain-enhancer of activated B cells) signaling pathway independently of its CFTR inhibitory action.
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 toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor. (Only for Reference)

Synonyms	CFTRinh 172, CFTR Inhibitor-172, CFTRinh-172, CFTRinh172
Molecular Weight	409.4
Formula	C18H10F3NO3S2
CAS No.	307510-92-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40.9 mg/mL (100 mM)

References and Literature

1. Ma T, et al. J Clin Invest. 2002, 110(11), 1651-1658. 2. Lu M, et al. Curr Eye Res. 2012, 37(8), 671-677. 3. Kelly M, et al. J Pharmacol Exp Ther. 2010, 333(1), 60-69. 4. Sawasvirojwong S, et al. PLoS Negl Trop Dis. 2013, 7(6), e2293.

Citations

1. Graeber S Y, Balázs A, Ziegahn N, et al.Personalized CFTR Modulator Therapy for G85E and N1303K Homozygous Patients with Cystic Fibrosis.International Journal of Molecular Sciences.2023, 24(15): 12365.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Covalent Inhibitor Library Ion Channel Inhibitor Library Autophagy Compound Library Anti-Fibrosis Compound Library Fluorochemical Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CFTR(inh)-172 307510-92-5 Autophagy Membrane transporter/Ion channel CFTR Cystic fibrosis transmembrane conductance regulator Inhibitor CFTRinh 172 CFTR Inhibitor-172 CFTRinh-172 CFTR(inh) 172 CFTR(inh)172 CFTRinh172 inhibit inhibitor

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