首页 Metabolism Hydroxylase Ketoconazole
Ketoconazole
编号 T0679     别名: (±)-Ketoconazol, R-41400, Extina, Xolegel
CAS 65277-42-1     分子式 C26H28Cl2N4O4     分子量 531.43
靶点: 12-hydroxylase; 17-hydroxylase; Cyclosporine oxidase; CYP24A1; CYP3A4; Steroid 21-hydroxylase; Testosterone 6 beta-hydroxylase;
Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
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规格 库存 单价 数量
50 mg 上海现货 283.00
100 mg 上海现货 417.00
200 mg 上海现货 630.00
500 mg 上海现货 1087.00
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生物活性

产品描述

Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

靶点活性

12-hydroxylase,

17-hydroxylase,

Cyclosporine oxidase,0.19mM

CYP24A1,

CYP3A4,

Steroid 21-hydroxylase,

Testosterone 6 beta-hydroxylase,0.22mM

实验溶液

30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

体外活性

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。

体内活性

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.

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

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)

细胞系: HT29-S-B6 colon cell

动物实验

动物模型:Wistar rats

化学信息

分子量

531.43

分子式

C26H28Cl2N4O4

CAS

65277-42-1

溶解度

DMSO: 9.4 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.882 ml 9.409 ml 18.817 ml
5 mM 0.376 ml 1.882 ml 3.763 ml
10 mM 0.188 ml 0.941 ml 1.882 ml
50 mM 0.038 ml 0.188 ml 0.376 ml
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