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Chemical Structure| 1004316-88-4 Chemical Structure| 1004316-88-4

Structure of Cobicistat
CAS No.: 1004316-88-4

Chemical Structure| 1004316-88-4

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Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

Synonyms: GS-9350

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Product Details of Cobicistat

CAS No. :1004316-88-4
Formula : C40H53N7O5S2
M.W : 776.02
SMILES Code : O=C(OCC1=CN=CS1)N[C@H](CC[C@@H](NC([C@@H](NC(N(CC2=CSC(C(C)C)=N2)C)=O)CCN3CCOCC3)=O)CC4=CC=CC=C4)CC5=CC=CC=C5
Synonyms :
GS-9350
MDL No. :MFCD18251449

Safety of Cobicistat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Vero E6 cells 2.5, 5, 10 µM 24 h Decreases replication-competent virus PMC8941859
T84 cells 5 to 10 µM 48 h Partially rescues viability of infected cells PMC8941859
Primary rat oligodendrocyte precursor cells 150 nM, 1.5 μM, 4 μM 72 h To examine the effect of Cobicistat on oligodendrocyte differentiation, results showed that Cobicistat did not significantly affect oligodendrocyte differentiation. PMC7736549
Human normal liver cells (HL-7702) 200 ng/mL 1 or 4 h To evaluate the cellular uptake ability of functionalized DTX-LNS, the results showed that the uptake of functionalized DTX-LNS in HepG2 cells was significantly higher than that in HL-7702 cells. PMC6489590

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Intracranial tumor xenograft model Oral gavage 10 mg/kg Not specified To evaluate the inhibitory effect of Cobicistat on tumor growth in glioblastoma xenograft models. The results showed that the combination of Cobicistat and TMZ significantly suppressed tumor growth and prolonged the survival of mice. PMC11697892
Balb/c mice Not used Oral 30 mg/kg Once daily for 8 days To study the effect of Cobicistat on B cell development, results showed that in 70% of the mice, Cobicistat combined with Elvitegravir significantly reduced the number of mature B lymphocytes. PMC5520896
Mice Lgr5CreERtdTomfl mice Oral 5 mg/kg Twice daily for 4 days To investigate the effect of reduced Wnt ligand secretion on stem cell dynamics, it was found that Wnt ligand inhibition reduced the number of stem cells in the stem cell pool and accelerated the fixation of monoclonal cells. PMC5859272
Syrian hamsters SARS-CoV-2 infection model Oral 50 mg/kg Once daily for 5 days Decreases viral load and mitigates disease progression PMC8941859
Mice Cuprizone-induced demyelination model Intravenous injection 65 mg/kg Once daily for three weeks To examine the effect of Cobicistat in combination with Elvitegravir on remyelination in mice, results showed that Cobicistat in combination with Elvitegravir inhibited remyelination. PMC7736549
Kunming mice H22 hepatocellular carcinoma mouse model Intravenous injection 5 mg/kg Every two days for three weeks To evaluate the in vivo antitumor efficacy of functionalized DTX-LNS, the results showed that functionalized DTX-LNS significantly inhibited tumor growth with low toxicity. PMC6489590

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03858491 Non Small Cell Lung Cancer EARLY_PHASE1 COMPLETED 2021-12-31 Maastricht University Medical ... More >>Centre, Maastricht, Limburg, 6225EC, Netherlands|Antoni van Leeuwenhoek hospital, Amsterdam, Noord-Holland, 1066CX, Netherlands Less <<
NCT05748093 Non-small Cell Lung Cancer PHASE4 RECRUITING 2026-09-01 MaastrichtUMC, Maastricht, Lim... More >>burg, 6229HX, Netherlands Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.29mL

0.26mL

0.13mL

6.44mL

1.29mL

0.64mL

12.89mL

2.58mL

1.29mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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