Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor - HCV Protease inhibitor Sofosbuvir For research use only.

Sofosbuvir

Synonyms: GS-7977, PSI-7977

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

Sofosbuvir Chemical Structure

Sofosbuvir Chemical Structure

CAS: 1190307-88-0

Selleck's Sofosbuvir has been cited by 39 publications

Purity & Quality Control

Batch: Purity: 99.92%
99.92

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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
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]
Cell Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05992077 Not yet recruiting HCV Infection ANRS Emerging Infectious Diseases August 7 2023 Not Applicable
NCT05140941 Recruiting Hepatitis C Chronic|Pregnancy; Infection Catherine Anne Chappell|Gilead Sciences|University of Pittsburgh April 4 2022 Phase 4
NCT04852614 Recruiting Hepatitis C Virus Infection Ain Shams University December 1 2020 --
NCT04773756 Completed Covid19 Alexandria University November 1 2020 Phase 4
NCT04382404 Completed Hepatitis C Chronic Catherine Anne Chappell|Gilead Sciences|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|University of Pittsburgh October 22 2020 Phase 1

Chemical lnformation & Solubility

Molecular Weight 529.45 Formula

C22H29FN3O9P
CAS No. 1190307-88-0 SDF Download Sofosbuvir SDF
Smiles CC(C)OC(=O)C(C)NP(=O)(OCC1C(C(C(O1)N2C=CC(=O)NC2=O)(C)F)O)OC3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (188.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 11 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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