Cat. No.: HY-10493

Cobicistat

(Synonyms: GS-9350)

12 Cited Publications

Customer Review

Based on 12 publication(s) in Google Scholar

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.

Purity: 99.49%
CAS No.: 1004316-88-4
Formula: C₄₀H₅₃N₇O₅S₂
Molecular Weight:776.02

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Cobicistat Chemical Structure

CAS No.: 1004316-88-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (12)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

CYP3

HIV-1

All Cytochrome P450 Isoforms :

All HIV Isoforms :

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1004316-88-4
Appearance Solid
Molecular Weight 776.02
Formula C₄₀H₅₃N₇O₅S₂
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
Synonyms

GS-9350
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

Publications (12)

All Cell Proliferation/Viability AssayWBIn Vivo ImagingHistological Imaging/StainingFlow Cytometry

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Journal Impact Factor

ACS Nano

Endolysosomal Sequestration Effects Controlled Release of BRAF Paradox Breaker Nanoparticles. [Abstract]

2025 Sep 30;19(38):33879-33890. PMID: 40954128
Acta Pharm Sin B

Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment. [Abstract]

2021 Jun;11(6):1607-1616. PMID: 34221871
Acta Pharm Sin B

Novel PF74-like small molecules targeting the HIV-1 capsid protein: Balance of potency and metabolic stability. [Abstract]

2021 Mar;11(3):810-822. PMID: 33777683
J Exp Clin Cancer Res

CYP3A5 promotes glioblastoma stemness and chemoresistance through fine-tuning NAD+/NADH ratio. [Abstract]

2025 Jan 3;44(1):3. PMID: 39754188

Cobicistat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]

Cell viability assay with the increasing concentrations of Cobicistat (Cobi) (1, 2, 4, 8, 16, 32, 64, 128 μM).

Cobicistat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]

Immunoblots of cleaved PARP, γH2AX, CD133, and PUMA in GSCs treated with Cobicistat (Cobi) and TMZ.

Cobicistat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]

Representative images of bioluminescence intensities of nude mice intracranially implanted with U87MG GSCs in treatment of DMSO, TMZ (5 mg/kg), Cobicistat (Cobi) (10 mg/kg) or TMZ (5 mg/kg) + Cobi (10 mg/kg) by gavage.

Cobicistat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]

Representative images of H&E staining of tumor sections in treatment of DMSO, TMZ (5 mg/kg), Cobicistat (Cobi) (10 mg/kg) or TMZ (5 mg/kg) + Cobi (10 mg/kg) by gavage.

Cobicistat purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]

Representative images and quantification of cell apoptosis measured by flow cytometry in treatment of DMSO, TMZ (5 mg/kg), Cobicistat (Cobi) (10 mg/kg) or TMZ (5 mg/kg) + Cobi (10 mg/kg) by gavage.
Eur J Med Chem

Novel HIV-1 capsid-targeting small molecules of the PF74 binding site. [Abstract]

2020 Oct 15;204:112626. PMID: 32814250
Eur J Med Chem

Chemical profiling of HIV-1 capsid-targeting antiviral PF74. [Abstract]

2020 Aug 15;200:112427. PMID: 32438252
Toxicol Sci

Targeting Xenobiotic Nuclear Receptors PXR and CAR to Prevent Cobicistat Hepatotoxicity. [Abstract]

2021 Apr 27;181(1):58-67. PMID: 33629115
Expert Opin Drug Metab Toxicol

In vitro- in vivo correlation of the drug-drug interaction potential of antiretroviral HIV treatment regimens on CYP1A1 substrate riociguat. [Abstract]

2019 Nov;15(11):975-984. PMID: 31619082
Cancer Res Commun

Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition. [Abstract]

2021 Nov;1(2):79-89. PMID: 34950932
Viruses

Toward Structurally Novel and Metabolically Stable HIV-1 Capsid-Targeting Small Molecules. [Abstract]

2020 Apr 16;12(4):452. PMID: 32316297
Chemrxiv

2021, Jun 10.
Drug Metab Lett

Biotransformation of Cobicistat: Metabolic Pathways and Enzymes. [Abstract]

2016;10(2):111-23. PMID: 26935921

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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 K_m 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.

MedChemExpress (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%.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lianhong Xu, et al. Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer. ACS Med. Chem. Lett., 2010, 1 (5), pp 209–213

[2]. Temesgen Z. Cobicistat, a pharmacoenhancer for HIV treatments. Drugs Today (Barc). 2013 Apr;49(4):233-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-COVID-19 Compound Library

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Drug-Induced Liver Injury (DILI) Compound Library

Mitochondria-Targeted Compound Library

Rare Diseases Drug Library

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Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Cobicistat

All Cytochrome P450 Isoforms

All HIV Isoforms

Biological Activity

Chemical Information

Publications (12)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Cobicistat Related Classifications

HY-10493 Related Classifications