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Cobicistat

产品编号 T6246 CAS 1004316-88-4

别名: Tybost, GS-9350, 考西司他

Cobicistat (GS-9350) 是一种细胞色素酶P450 3A 的选择性抑制剂，IC50值为30-285 nM。它是一种药代动力学增强剂，可增强抗 HIV 药物的吸收。

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Cobicistat, CAS 1004316-88-4

规格	价格/CNY	货期
1 mg	￥ 367	现货
2 mg	￥ 525	现货
5 mg	￥ 823	现货
10 mg	￥ 1,230	现货
25 mg	￥ 2,260	现货
50 mg	￥ 3,730	现货
100 mg	￥ 5,390	现货
1 mL * 10 mM (in DMSO)	￥ 1,060	现货

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选择批次

纯度: 99.62%

纯度: 99.51%

纯度: 99.43%

纯度: 97.79%

纯度: 97.36%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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.
靶点活性	CYP3A:30 nM-285 nM
体外活性	Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes as a pharmacoenhancer. GS-9350 inhibits CYP3A with IC50 spectrum from 30 nM to 285 nM. In contrast to ritonavir, GS-9350 is devoid of anti-HIV activity, with IC50 of > 30 μM against HIV-1 protease and EC50 of > 30 μM in MT-2 HIV infection assay, and is thus more suitable for use in boosting anti-HIV drugs without risking selection of potential drug-resistant HIV variants. GS-9350 shows reduced liability for drug interactions and may have potential improvements in tolerability over ritonavir. [1]
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.
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%.

别名	Tybost, GS-9350, 考西司他
分子量	776.02
分子式	C40H53N7O5S2
CAS No.	1004316-88-4

存储

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

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)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.2886 mL	6.4431 mL	12.8863 mL	32.2157 mL
	5 mM	0.2577 mL	1.2886 mL	2.5773 mL	6.4431 mL
	10 mM	0.1289 mL	0.6443 mL	1.2886 mL	3.2216 mL
	20 mM	0.0644 mL	0.3222 mL	0.6443 mL	1.6108 mL
	50 mM	0.0258 mL	0.1289 mL	0.2577 mL	0.6443 mL
	100 mM	0.0129 mL	0.0644 mL	0.1289 mL	0.3222 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Xu L, et al. ACS Med. Chem. Lett, 2010, 1(5), 209-213.

文献引用

1. Yan F, Gao F. An overview of potential inhibitors targeting non-structural proteins 3 (PLpro and Mac1) and 5 (3CLpro/Mpro) of SARS-CoV-2. Computational and Structural Biotechnology Journal. 2021, 19: 4868.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Cobicistat 1004316-88-4 Metabolism Microbiology/Virology Proteases/Proteasome P450 HIV Protease Inhibitor HIV Human immunodeficiency virus antiviral HIV-1 Tybost Cytochrome P450 GS-9350 CYPs GS 9350 考西司他 CYP3A GS9350 inhibit inhibitor

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Cobicistat

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords