Ketoconazole

製品コードS1353 バッチS135304

印刷

化学情報

Chemical Structure Synonyms R 41400 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H28Cl2N4O4
分子量 531.43 CAS No. 65277-42-1
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 19 mg/mL (35.75 mM)
Ethanol 12 mg/mL (22.58 mM)
Water 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
30%propylene glycol 5%Tween80 65%D5W

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。

 30.000mg/ml (56.45mM) Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
10%DMSO 40%PEG300 5%TWEEN80 45%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。

 3.500mg/ml (6.59mM) Taking the 1 mL working solution as an example, add 100 μL of 35 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 clarify; then continue to add 450 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 Ketoconazoleは、シクロスポリンオキシダーゼおよびテストステロン6β-ヒドロキシラーゼをそれぞれIC50 0.19 mMおよび0.22 mMで阻害します。Ketoconazoleはandrogen生合成阻害剤です。
in vitro Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. This compound competes for [3H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM. It reduces cell proliferation and [3H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. This chemical inhibits the incorporation of [3H]thymidine with IC50 of 2 μM and 13 μM in the Evsa-T cell line and MDA-MB-231 cell line, respectively. It induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells. It is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL.
in vivo Ketoconazole (25 mg/kg, i.p.) significantly decreases plasma corticosterone and reduces low dose cocaine self-administration without affecting food-reinforced responding in rats. This compound raises the AUC of orally administered digoxin from 63 mg x h/L to 411 mg x h/L in rats. It raises the AUC of intravenously administered digoxin from 93 mg × h/L to 486 mg × h/L in rats. This chemical increases digoxin bioavailability from 0.68 to 0.84 in rats, while mean absorption time is reduced from 1.1 hours to 0.3 hour.
特徴 More active than both Econazole and Miconazole against Malassezia species.

プロトコル(参考用のみ)

キナーゼアッセイ Whole Cell [3H]R1881 Binding Assay
Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
細胞アッセイ 細胞株 HT29-S-B6 colon cell
濃度 25 μM
反応時間 72 hours
実験の流れ HT29-S-B6 cells (5×105) are plated in 35-mm Petri dishes. The next day, the medium is changed and effectors are added in a small volume (10-20 μL). The incubation medium is renewed every day during the experiments. The same triplicate dishes are used for cell counts, [3H]thymidine incorporation, and flow cytometry. [3H]Thymidine (0.5 μCi) is allowed to incorporate for 24 hours; at the end of incubation, cells are rinsed with 1 mL of medium, detached with 1 mL of trypsin-EDTA, and diluted (1:3) with the culture medium. An aliquot (0.5-1 mL) is used for cell count with a Coulter Counter.
動物実験 動物モデル male Wistar rats
投薬量 25 mg/kg
投与方法 Intraperitoneal injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/11309497/
  • https://pubmed.ncbi.nlm.nih.gov/1526623/
  • https://pubmed.ncbi.nlm.nih.gov/1458471/
  • https://pubmed.ncbi.nlm.nih.gov/10792228/
  • https://pubmed.ncbi.nlm.nih.gov/10933341/
  • https://pubmed.ncbi.nlm.nih.gov/9654217/

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：

Adenosine signalling drives antidepressant actions of ketamine and ECT [ Nature, 2025, 10.1038/s41586-025-09755-9] PubMed: 41193806
CRISPR targeting of FOXL2 c.402C>G mutation reduces malignant phenotype in granulosa tumor cells and identifies anti-tumoral compounds [ Mol Oncol, 2025, 10.1002/1878-0261.13799] PubMed: 39776254
Pralatrexate represses the resistance of HCC cells to molecular targeted agents via the miRNA-34a/Notch pathway [ Discov Oncol, 2024, 15(1):709] PubMed: 39585461
NFX1-123: A potential therapeutic target in cervical cancer [ J Med Virol, 2023, 95(6):e28856] PubMed: 37288708
TPX2 enhances the transcription factor activation of PXR and enhances the resistance of hepatocellular carcinoma cells to antitumor drugs [ Cell Death Dis, 2023, 14(1):64] PubMed: 36707511
Hexokinase 2 confers radio-resistance in hepatocellular carcinoma by promoting autophagy-dependent degradation of AIMP2 [ Cell Death Dis, 2023, 14(8):488] PubMed: 37524692
Genetically engineered human pituitary corticotroph tumor organoids exhibit divergent responses to glucocorticoid receptor modulators [ Transl Res, 2023, S1931-5244(23)00002-6] PubMed: 36640905
Quantitative chemometric phenotyping of three-dimensional liver organoids by Raman spectral imaging [ Cell Rep Methods, 2023, 3(4):100440] PubMed: 37159662
Quantitative chemometric phenotyping of three-dimensional liver organoids by Raman spectral imaging [ Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440] PubMed: None
Integration of glucose and cardiolipin anabolism confers radiation resistance of HCC [ Hepatology, 2022, 75(6):1386-1401] PubMed: 34580888

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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