CFTRinh-172

製品コードS7139 バッチS713902

印刷

化学情報

Chemical Structure Synonyms CFTR inhibitor 172 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H10F3NO3S2
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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 9.000mg/ml (21.98mM) Taking the 1 mL working solution as an example, add 50 μL of 180 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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] This compound, as a selective CFTR channel inhibitor, also completely abolishes the Cl− current in the rabbit acinar and duct cells of rabbit lacrimal gland. [2] It 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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–.
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 of this compound.
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

参考

  • https://pubmed.ncbi.nlm.nih.gov/12464670/
  • https://pubmed.ncbi.nlm.nih.gov/22578307/
  • https://pubmed.ncbi.nlm.nih.gov/20051483/
  • https://pubmed.ncbi.nlm.nih.gov/23826402/

カスタマーフィードバック

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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identity, functional consequences, and context effects of amino acids inserted during suppression of CFTR nonsense mutations [ J Cyst Fibros, 2025, S1569-1993(25)01612-1] PubMed: 41015699
Efferocytosis reprograms the tumor microenvironment to promote pancreatic cancer liver metastasis [ Nat Cancer, 2024, 10.1038/s43018-024-00731-2] PubMed: 38355776
Inhibiting CFTR through inh-172 in primary neutrophils reveals CFTR-specific functional defects [ Sci Rep, 2024, 14(1):31237] PubMed: 39732786
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
Investigation of precision therapies for splice variants [ Johns Hopkins University, 2022, ] PubMed: None

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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