|
受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
|
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) | 11 mg/mL (20.69 mM) | ||||
| Ethanol | 8 mg/mL (15.05 mM) | ||||||
| Water | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
|
||||||
|
* <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 inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor. |
|---|---|
| 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. [2] 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. [3] It is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. [4] |
| 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. [5] 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. [6] |
| 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
|
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：
| 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 |
| 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 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 |
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。