Sofosbuvir

Catalog No.S2794 Batch:S279403

Technical Data

Formula

C₂₂H₂₉FN₃O₉P

Molecular Weight

529.45

CAS No.

1190307-88-0

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (188.87 mM)

Ethanol

25 mg/mL (47.21 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	1.6mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Sofosbuvir is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.

Targets

NS5B polymerase ^[1]

In vitro

As HCV NS5B polymerase inhibitor, PSI-7977 displays more potent inhibitory activity against HCV RNA replication than PSI-7976 with EC50 of 92 nM versus 1.07 μM and EC90 of 0.29 μM versus 2.99 μM, consistent with that incubating clone A cells with PSI-7977 leads to a higher concentration of PSI-7409 than clone A cells incubated with PSI-7976. PSI-7977 is an effective substrate for CatA to form PSI-352707 with 18-30 fold more potency as compared with PSI-7976. Unlike GS-7976, however, the CES1-mediated hydrolysis of PSI-7977 does not progress in a time-dependent manner. ^[1] The S282T NS5B polymerase mutation but not S96T mutation confers resistance to PSI-7977 with EC90 increases from 0.42 μM to 7.8 μM. When assessed in an 8-day cytotoxicity assay, PSI-7977 displays no cytotoxicity against Huh7, HepG2, BxPC3, and CEM cells even at concentrations up to 100 μM. PSI-7977 treatment for 14 days shows a IC90 of 72.1 μM and 68.6 μM for the inhibition of mtDNA and rDNA, respectively, in HepG2 cells. ^[2] PSI-7977 exhibits potent activity against genotype (GT) 1a, 1b, and 2a (strain JFH-1) replicons and chimeric replicons containing GT 2a (strain J6), 2b, and 3a NS5B polymerase. Sequence analysis of the JFH-1 NS5B region indicates that additional amino acid changes including T179A, M289L, I293L, M434T, and H479P are selected both prior to and after the emergence of S282T, which are required to confer resistance to PSI-7977. ^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Huh7, HepG2, BxPC3, and CEM Concentrations Dissolved in DMSO, final concentrations ~100 μM Incubation Time 8 days Method Cells are exposed to various concentrations of PSI-7977 for 8 days. At the end of the growth period, MTS dye from the CellTiter 96 AQueous One Solution Cell Proliferation Assay kit is added to each well, and the plate is incubated for an additional 2 hours. The absorbance at 490 nm is read with a Victor3 plate reader using themedium only controlwells as blanks. The 50% inhibition value (IC50) is determined by comparing the absorbance in wells containing cells and PSI-7977 to untreated cell control wells.

Cell Assay:^{^[2]}

Cell lines
Huh7, HepG2, BxPC3, and CEM
Concentrations
Dissolved in DMSO, final concentrations ~100 μM
Incubation Time
8 days
Method
Cells are exposed to various concentrations of PSI-7977 for 8 days. At the end of the growth period, MTS dye from the CellTiter 96 AQueous One Solution Cell Proliferation Assay kit is added to each well, and the plate is incubated for an additional 2 hours. The absorbance at 490 nm is read with a Victor3 plate reader using themedium only controlwells as blanks. The 50% inhibition value (IC50) is determined by comparing the absorbance in wells containing cells and PSI-7977 to untreated cell control wells.

References

Customer Product Validation

: Data from [Data independently produced by , , Hepatology, 2017, 66(3):758-771]

: Data from [Data independently produced by , , Antimicrob Agents Chemother, 2016, 60(6):3786-3793.]

: Data from [Data independently produced by , , PLoS One, 2018, 13(11):e0198226]

Selleck's Sofosbuvir has been cited by 44 publications

Hepatitis C virus-induced differential transcriptional traits in host cells after persistent infection elimination by direct-acting antivirals in cell culture [ J Med Virol, 2024, 96(7):e29787]	PubMed: 38988177
Immortalized hepatocyte-like cells: A competent hepatocyte model for studying clinical HCV isolate infection [ PLoS One, 2024, 19(5):e0303265]	PubMed: 38739590
Hepatitis C virus infects and perturbs liver stem cells [ mBio, 2023, 10.1128/mbio.01318-23]	PubMed: 37938000
Activation of the urotensin-II receptor by remdesivir induces cardiomyocyte dysfunction [ Commun Biol, 2023, 6(1):511]	PubMed: 37173432
Fitness-Dependent, Mild Mutagenic Activity of Sofosbuvir for Hepatitis C Virus [ Antimicrob Agents Chemother, 2023, 67(7):e0039423]	PubMed: 37367486
ヒト iPS 細胞由来心筋細胞を用いた慢性収縮毒性評価法の開発 [ Okayama University, 2023 , 10.18926/65391]	PubMed: none
An anti-influenza A virus microbial metabolite acts by degrading viral endonuclease PA [ Nat Commun, 2022, 13(1):2079]	PubMed: 35440123
Therapeutic targeting of organelles for inhibition of Zika virus replication in neurons [ Antiviral Res, 2022, S0166-3542(22)00233-9]	PubMed: 36396026
Efficacy decrease of antiviral agents when administered to ongoing hepatitis C virus infections in cell culture [ Front Microbiol, 2022, 13:960676]	PubMed: 35992670
Processing and Subcellular Localization of the Hepatitis E Virus Replicase: Identification of Candidate Viral Factories [ Front Microbiol, 2022, 13:828636]	PubMed: 35283856

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.