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

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.

For research use only. We do not sell to patients.

Cobicistat Chemical Structure

Cobicistat Chemical Structure

CAS No. : 1004316-88-4

Size Price Stock Quantity
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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 141 In-stock
Solution
10 mM * 1 mL in DMSO USD 141 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 165 In-stock
50 mg USD 495 In-stock
100 mg USD 715 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Cobicistat:

Cobicistat Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

CYP3

 

HIV-1

 

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].

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

Cobicistat Related Antibodies
Clinical Trial
Molecular Weight

776.02

Formula

C40H53N7O5S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CN(C(N[C@@H](CCN1CCOCC1)C(N[C@@H](CC2=CC=CC=C2)CC[C@@H](NC(OCC3=CN=CS3)=O)CC4=CC=CC=C4)=O)=O)CC5=CSC(C(C)C)=N5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (322.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.77%

COA (249 KB) LCMS (122 KB)

Handling Instructions (2659 KB)
References
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.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 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
15 mM 0.0859 mL 0.4295 mL 0.8591 mL 2.1477 mL
20 mM 0.0644 mL 0.3222 mL 0.6443 mL 1.6108 mL
25 mM 0.0515 mL 0.2577 mL 0.5155 mL 1.2886 mL
30 mM 0.0430 mL 0.2148 mL 0.4295 mL 1.0739 mL
40 mM 0.0322 mL 0.1611 mL 0.3222 mL 0.8054 mL
50 mM 0.0258 mL 0.1289 mL 0.2577 mL 0.6443 mL
60 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5369 mL
80 mM 0.0161 mL 0.0805 mL 0.1611 mL 0.4027 mL
100 mM 0.0129 mL 0.0644 mL 0.1289 mL 0.3222 mL
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Cobicistat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cobicistat1004316-88-4GS-9350GS9350GS 9350Cytochrome P450HIVCYPsHuman immunodeficiency virusantiviralHIV-1CYP3AInhibitorinhibitorinhibit

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