酮康唑 T0679

Product Introduction
Bioactivity


英文名: Ketoconazole

描述: Ketoconazole (R-41400) 是一种咪唑类抗真菌剂，也是一种 CYP3A4 抑制剂。

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: 腹腔注射Ketoconazole（25 mg/kg）后,大鼠体内血浆皮质酮浓度明显降低,也可使低剂量可卡因自我给药减少.Ketoconazole处理组大鼠,地高辛生物有效性得到提高,从0.68提高至0.84 ,而平均吸收时间从1.1 h减少至0.3 h.此外,地高辛的口服AUC值也得到提高,从63 mg·h/L提高至411 mg·h/L.地高辛的静脉注射AUC值也被提高,从93 mg·h/L提高至486 mg·h/L.

体内活性: 在HT29-S-B6结肠癌细胞中,Ketoconazole剂量依赖性地降低细胞增殖,[3H]胸苷渗透,IC50为2.5 mM。在Evsa-T细胞系和MDA-MB-231 细胞系中,Ketoconazole抑制[3H]胸苷渗透,IC50 分别为2 μM 和13 μM。在HT29-S-B6细胞中,Ketoconazole在24 h内,剂量依赖性地诱导S期细胞数减少（从17%降低至3%）,Go-G1期细胞百分数则相应增加（从64% 增加至80%）。通过与[3H]Dexamethasone竞争性结合的方式,Ketoconazole能够抑制成纤维细胞糖皮质激素受体,IC50为0.3 mM。几种马拉色霉菌种对Ketoconazole较为敏感,最小抑制浓度为0.03 μg/mL。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5.31 mg/mL (10 mM)


关键字: Inhibitor | Ketoconazole | inhibit | Fungal | Cytochrome P450 | R 41400 | Ras | Ketoconazol | CYPs | R41400

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相关库: FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | GPCR Compound Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途