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 is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.
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. [1] Benzethonium chloride inhibits muscarinic signaling with a calculated IC50 of 15 μM and a Hill coefficient of 0.6. [3] 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. [4] 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. [5]

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. [5]

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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