1. Metabolic Enzyme/Protease
    Anti-infection
  2. Cytochrome P450
    HIV
  3. Cobicistat

Cobicistat (Synonyms: GS-9350)

目录号: HY-10493 纯度: 98.05%
产品使用指南

Cobicistat 是有效,选择性的细胞色素酶 P450 3A (CYP3A) 抑制剂,IC50 值为30-285 nM。 Cobicistat 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 Chemical Structure

Cobicistat Chemical Structure

CAS No. : 1004316-88-4

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.

IC50 & Target

IC50: 30-285 nM (Cytochrome P450)[1]

体外研究
(In Vitro)

In HIV-1 protease enzymatic assay and antiviral cellular assays. Cobicistat is inactive against HIV-1 protease (IC50>30 μM) . And Cobicistat has no inhibitory effect against HIV replication in a multicycle 5-day MT-2 HIV infection assay (EC50>30 μM). In assays using MT-2 cells, Cobicistat exhibits minimal cytotoxicity, with a CC50 value above 80 μM[1].
The mode of inhibition of human CYP3A by Cobicistat and Ritonavir shares the same mechanism of action for the inhibition of CYP3A. It shows its inhibitory effects on CYP3A may involve directly at the heme group of the CYP3A enzyme[1].
The minimal adverse effects of Cobicistat in these assays suggest a lower potential for toxicity related to altered lipid metabolism.
In the lipid accumulation assay with the human adipocytes, Ritonavir shows a clear effect with an EC50 of 16 μM. However, Cobicistat exhibits no effect at a concentration up to 30 μM[1].
In the glucose uptake assay with mouse adipocytes, Ritonavir shows a pronounced effect at the concentration of 10 μM. In contrast, the effects on glucose uptake by Cobicistat (10 μM) is significantly less[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

776.02

Formula

C40H53N7O5S2

CAS 号
中文名称

可比司他;科比司他;可比西他;考西司他;考比泰特

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (322.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2886 mL 6.4431 mL 12.8863 mL
5 mM 0.2577 mL 1.2886 mL 2.5773 mL
10 mM 0.1289 mL 0.6443 mL 1.2886 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.68 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Kinase Assay
[1]

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°C and the reaction initiated by the addition of an NADPH generating system followed by further incubation at 37°C 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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%.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

纯度: 99.77%

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产品名称:
Cobicistat
目录号:
HY-10493
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