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Synonyms | CFTR inhibitor 172 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H10F3NO3S2 |
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分子量 | 409.4 | CAS No. | 307510-92-5 | ||||
Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (200.29 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | 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. |
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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] |
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] |
キナーゼアッセイ | Screening procedures | |
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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–. | ||
細胞アッセイ | 細胞株 | Fischer rat thyroid (FRT) cells |
濃度 | ~1 mM | |
反応時間 | 24 hours | |
実験の流れ | Cell toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor. |
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動物実験 | 動物モデル | An adult mouse model of Vibrio cholerae-induced diarrhea |
投薬量 | 20 µg/6 h | |
投与方法 | Intraperitoneal administration |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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