Benzethonium Chloride

製品コードS4162 バッチS416201

印刷

化学情報

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

C27H42NO2.Cl
分子量 448.08 CAS No. 121-54-0
Solubility (25°C)* 体外 DMSO 90 mg/mL (200.85 mM)
Water 90 mg/mL (200.85 mM)
Ethanol 90 mg/mL (200.85 mM)
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
2%DMSO 40%peg300 2%tween 56%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。

 0.300mg/ml (0.67mM) Taking the 1 mL working solution as an example, add 20 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 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 Benzethonium chlorideはnAChRsの強力な阻害剤であり、α4β2 nAChRsおよびα7 nAChRsをそれぞれ49 nMおよび122 nMのIC50で阻害します。
in vitro

Benzethonium chloride inhibits the α7 nAChRs in a mixed competitive and non-competitive manner but there is no voltage- or use-dependence of the response in either subtype. Benzethonium chloride inhibits muscarinic signaling with a calculated IC50 of 15 μM and a Hill coefficient of 0.6. Benzethonium (5 μM) significantly increases cytosolic Ca(2+)-concentration, decreases forward scatter and triggered annexin V-binding affecting some 30% of the erythrocytes. Benzethonium (5 μM) further significantly enhances the effect of glucose depletion on cytosolic Ca(2+)-concentration and annexin V-binding, but significantly blunts the effect of glucose depletion on forward scatter. Benzethonium (5 μM) significantly enhances lactic acid formation but not ceramide abundance. Benzethonium chloride reduces cell viability with IC50 of 3.8 μM in FaDu, 42.2 μM in NIH 3T3, 5.3 μM in C666-1, and 17.0 μM in GM05757. Benzethonium chloride (9 μM) induces apoptosis and activates caspases after 12 hours in FaDu cells.

in vivo

Benzethonium chloride (5 mg/kg) ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors, and combined additively with local tumor radiation therapy in established FaDu tumors in SCID mice.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 FaDu, C666-1, NIH 3T3 and GM05757 cell lines
濃度 42.2 μM
反応時間 48 hours
実験の流れ

Cells are seeded in 96-well plates at 5,000 per well in 100 μL of growth medium and allowed to incubate for 24 hours. Benzethonium chloride is then added, as indicated, in a total volume of 5 μL. After 48 hours, MTS assay is done according to the specifications of the manufacturer, with DMSO (0.1%)–treated cells as negative control.
動物実験 動物モデル established FaDu tumors in SCID mice.
投薬量 5 mg/kg
投与方法 intraperitoneal injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/11606328/
  • https://pubmed.ncbi.nlm.nih.gov/9298350/
  • https://pubmed.ncbi.nlm.nih.gov/9197302/
  • https://pubmed.ncbi.nlm.nih.gov/21865743/
  • https://pubmed.ncbi.nlm.nih.gov/17000693/

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：

The liver microenvironment orchestrates FGL1-mediated immune escape and progression of metastatic colorectal cancer [ Nat Commun, 2023, 10.1038/s41467-023-42332-0] PubMed: 37872170
The liver microenvironment orchestrates FGL1-mediated immune escape and progression of metastatic colorectal cancer [ Nat Commun, 2023, 14(1):6690] PubMed: 37872170
Targeting CD36 determines nicotine derivative NNK-induced lung adenocarcinoma carcinogenesis [ iScience, 2023, 26(8):107477] PubMed: 37599821
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] PubMed: 36230806
Eryptosis and Malaria: New Experimental Guidelines and Re-Evaluation of the Antimalarial Potential of Eryptosis Inducers [ Front Cell Infect Microbiol, 2021, 11:630812] PubMed: 33777843
Benzethonium chloride suppresses lung cancer tumorigenesis through inducing p38-mediated cyclin D1 degradation. [ Am J Cancer Res, 2019, 9(11):2397-2412] PubMed: 31815042

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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