酮康唑|T0679

Ketoconazole
65277-42-1

￥655 500mg 起订

￥298 50mg 起订

￥418 100mg 起订

上海更新日期：2025-03-12

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 酮康唑

英文名称：: Ketoconazole

CAS号：: 65277-42-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.62%

产品类别：: 抑制剂

货号：: T0679

Product Introduction

Bioactivity

名称	Ketoconazole
描述	Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
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 \| Shipping with blue ice.
溶解度	DMSO : 5.31 mg/mL (10 mM), Sonication is recommended.
关键字	Inhibitor \| Ketoconazole \| inhibit \| Fungal \| Cytochrome P450 \| R 41400 \| Ras \| Ketoconazol \| CYPs \| R41400
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相关库	抑制剂库 \| 经典已知活性库 \| 抗真菌库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| GPCR靶点分子库 \| 膜蛋白靶向化合物库 \| FDA 上市激酶抑制剂库 \| 抗癌临床化合物库 \| 抗癌药物库

酮康唑|||Xolegel|||R-41400|||Extina|||(±)-Ketoconazol|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子