| 中文名称： |
酮康唑 |
| 英文名称: |
Ketoconazole |
| 产品分类： |
小分子化合物(化合物库) |
| CAS号： |
65277-42-1 |
| 分子式： |
C26H28CL2N4O4 |
| 分子量： |
531.43 |
*产品基础信息：
【产品中文名称】酮康唑;
【产品英文名称】Ketoconazole;
【纯度指标】99.95%;
【品牌】TargetMol;
【CAS号】65277-42-1;
【浓度】;
Product Introduction
Bioactivity
| 名称 | Ketoconazole |
| 描述 | Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1). |
| 细胞实验 | 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.(Only for Reference) |
| 激酶实验 | 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 |
| 体外活性 | 方法：人肝微粒体加入 Ketoconazole（0.3， 1， 2， 3， 5， 10 μM） 与 CYP3A 特异性底物睾酮和咪达唑仑 37°C 共孵育。高效液相色谱测定代谢产物（6β-羟基睾酮和 1'-羟基咪达唑仑）生成量。
结果：Ketoconazole 形式均能剂量依赖性抑制 CYP3A 活性，10 μM 时抑制至 3%（睾酮）以下。[1]
方法：胶质瘤细胞系 U87，患者来源的胶质瘤干细胞 GSCs 中加入浓度梯度（ 0.1-100 μM）Ketoconazole 处理 48-72 小时，Annexin V/PI 染色检测细胞增殖与凋亡。
结果：Ketoconazole 处理导致细胞增殖减少，凋亡比例增加。[2] |
| 体内活性 | 方法：将 U87-luc 细胞或患者来源的 GSC 原位接种于免疫缺陷小鼠大脑。待肿瘤形成后，随机分组开始给药。每日腹腔注射 Ketoconazole(50 mg/kg)或溶剂对照，连续治疗 4 周。通过生物发光成像监测肿瘤生长，并记录小鼠生存期。
结果：Ketoconazole 组小鼠肿瘤生长显著抑制，小鼠生存期显著延长。 肿瘤组织学分析显示，肿瘤细胞增殖减少，凋亡增加，且肿瘤代谢活性降低。[2]
方法：野生型小鼠腹腔注射 Ketoconazole(50 mg/kg)，约 30 分钟后静脉注射放射性示踪剂([¹¹C]洛哌丁胺或[¹¹C]dLop)，注射示踪剂后 30 分钟 处死小鼠，采集血液和全脑样本。
结果：Ketoconazole(50 mg/kg，i.p.)在体内能部分抑制[¹¹C]洛哌丁胺的 N-脱甲基代谢，提高了其血浆浓度，并减少了极性代谢物进入大脑。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.53 mg/mL (1 mM), Solution.
DMSO : 25 mg/mL (47.04 mM), Sonication and heating are recommended.
|
| 关键字 | Testosterone 6 beta-hydroxylase | Steroid 21-hydroxylase | Ras | R41400 | R 41400 | NADPHoxidase | Ketoconazole | Ketoconazol | Inhibitor | inhibit | Fungal | Cytochrome P450 | CYPs | CYP3A4 | CYP24A1 | Cyclosporine oxidase | 17-hydroxylase | 12-hydroxylase |
| 相关产品 | Calcium Propionate | Benzyl propionate | Levulinic acid | Doxycycline | Neomycin sulfate | Terbinafine hydrochloride | Chitosan hydrochloride (80%-90% deacetylated) | Dimethyl sulfoxide | Hyaluronic acid sodium (MW 20 kDa) | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | Anti-Aging Compound Library | GPCR Compound Library | Membrane Protein-targeted Compound Library | Immunology/Inflammation Compound Library | Pain-Related Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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