考西司他|T6246|TargetMol

Cobicistat
1004316-88-4

￥367 1mg 起订

￥525 2mg 起订

￥823 5mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 考西司他

英文名称：: Cobicistat

CAS号：: 1004316-88-4

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：: T6246

Product Introduction

Bioactivity

名称	Cobicistat
描述	Cobicistat (GS-9350) is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS.
细胞实验	Five-fold serial dilutions of the tested compounds are prepared in triplicate in 96-well plates. MT-2 cells are added to plates at a density of 20,000/well in a final assay volume of 200 μL. After a 5-day incubation at 37°C, the cytotoxic effect is determined using a cell viability assay. One hundred μL media is removed from each well and replaced with 100 μL of phosphate-buffered saline containing 1.7 mg/mL XTT and 5 μg/mL PMS. Following 1-hour incubation at 37°C, 20 μL of 2% Triton X- 100 is added to each well and absorbance is read at 450 nm with a background subtraction at 650 nm. The data are plotted as cell viability vs. drug concentration. Cell viability is expressed as a percentage of the signal from untreated samples (0% cytotoxicity) after the subtraction of signal from samples treated with 10 μM of Podophyllotoxin (100% cytotoxicity). The CC50 value is calculated from the inhibition plots as the concentration of drug which inhibits cell proliferation by 50%.
激酶实验	Cytochrome P450 Inhibition: Inhibition of human cytochrome P450 activities is determined in duplicate in pooled human hepatic microsomal fractions following current scientific and regulatory guidelines. Reaction conditions are linear with respect to incubation time and hepatic microsomal protein concentration. Substrates are present at concentrations equal to or less than their respective Km values determined under the same reaction conditions. Metabolite and/or substrate concentrations are determined using specific, internal standard controlled HPLC MS/MS assays. For reactions monitoring metabolite formation there is less than 20% consumption of substrate during the reaction. Unless otherwise noted microsomal fraction, diluted in potassium phosphate buffer, is preincubated with substrate and inhibitor for 5 min at 37 ℃ and the reaction initiated by the addition of an NADPH generating system followed by further incubation at 37 ℃ with shaking. Enzyme-selective positive control inhibitors are tested in parallel. At appropriate times aliquots of the mixture are removed and the reaction terminated by addition to a mixture of methanol and acetonitrile containing the respective internal standard. After centrifugation aliquots of the supernatant are subjected to HPLC-MS/MS analysis.
体外活性	Cobicistat（GS-9350）是一种高效且选择性的人类细胞色素P450 3A（CYP3A）酶的抑制剂，用作药效增强剂。GS-9350对CYP3A的抑制作用的IC50范围为30 nM至285 nM。与ritonavir不同，GS-9350不具备抗HIV活性，其对HIV-1蛋白酶的IC50 > 30 μM，以及在MT-2 HIV感染测定中的EC50 > 30 μM，因此在增强抗HIV化合物效果时，不会增加潜在耐药HIV变体的选择风险，更适合使用。GS-9350减少了药物相互作用的可能性，并可能在耐受性方面比ritonavir有所改进。[1]
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 : 93 mg/mL (119.8 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 93 mg/mL (119.8 mM)
关键字	Inhibitor \| Cobicistat \| HIV \| Human immunodeficiency virus \| antiviral \| HIV-1 \| Cytochrome P450 \| CYPs \| GS 9350 \| CYP3A \| GS9350 \| inhibit
相关产品	Tenofovir \| Naringin \| Valproic Acid \| Emtricitabine \| Lamivudine \| 5-Fluorouracil \| Decanedioic acid \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Naringenin \| Kaempferol \| Dimethyl fumarate
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌上市药物库 \| 已知活性化合物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 抗病毒库 \| 抗癌临床化合物库 \| 抗癌药物库

考西司他|||Tybost|||GS-9350|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