Elexacaftor (VX-445)

製品コードS8851 バッチS885101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C26H34F3N7O4S
分子量 597.65 CAS No. 2216712-66-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (167.32 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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 95% Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. 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 Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector.This is a compound which is not chiral purity.
in vitro

The pendrin-dependent increase in cystic fibrosis transmembrane conductance regulator (CFTR) current is additive with the CFTR modulator elexacaftor.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human bronchial epithelial cells from DeltaF508/DeltaF508 Cystic Fibrosis patients (CF HBECs)
濃度 3 µM
反応時間 48 h
実験の流れ

Using Chamber recordings from DeltaF508/DeltaF508 CF HBEC epithelia were treated with the LIE triple combination (1 µM Lumacaftor +0.02 µM Ivacaftor +3 µM Elexacaftor) for 48 h plus and minus 10 ng/mL IL-13 and/or 10 micromol/L niflumic acid (for 30 minutes) again. Transepithelial current (Isc) and conductance (Gt) were measured.

(Data sourced from selleck products)

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：

PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR [ Eur J Pharmacol, 2024, 967:176390] PubMed: 38336013
General trends in the effects of VX-661 and VX-445 on the plasma membrane expression of clinical CFTR variants [ Cell Chem Biol, 2023, S2451-9456(23)00125-3] PubMed: 37253358
ABC-transporter CFTR folds with high fidelity through a modular, stepwise pathway [ Cell Mol Life Sci, 2023, 80(1):33] PubMed: 36609925
A Novel Co-Culture Model Reveals Enhanced CFTR Rescue in Primary Cystic Fibrosis Airway Epithelial Cultures with Persistent Pseudomonas aeruginosa Infection [ Cells, 2023, 10.3390/cells12222618] PubMed: 37998353
UBE3C Facilitates the ER-Associated and Peripheral Degradation of Misfolded CFTR [ Cells, 2023, 12(23)2741] PubMed: 38067172
Elexacaftor Mediates the Rescue of F508del CFTR Functional Expression Interacting with MSD2 [ Int J Mol Sci, 2023, 10.3390/ijms241612838] PubMed: 37629017
Putting bicarbonate on the spot: pharmacological insights for CFTR correction in the airway epithelium [ Front Pharmacol, 2023, 14:1293578] PubMed: 38149052
The COPD-Associated Polymorphism Impairs the CFTR Function to Suppress Excessive IL-8 Production upon Environmental Pathogen Exposure [ Int J Mol Sci, 2023, 24(3)2305] PubMed: 36768629
Elexacaftor Mediates the Rescue of F508del CFTR Functional Expression Interacting with MSD2 [ Int J Mol Sci, 2023, 24(16)12838] PubMed: 37629017
TGF-β1 inhibition of ACE2 mediated by miRNA uncovers novel mechanism of SARS-CoV-2 pathogenesis [ J Innate Immun, 2023, 15(1):629-46] PubMed: 37579743

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。