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Sofosbuvir (GS-7977)

Name: Sofosbuvir (GS-7977)
Brand: Selleck Chemicals
SKU: S2794
Rating: 5 (34 reviews)

Catalog No.S2794 Synonyms: PSI-7977

For research use only.

Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.

CAS No. 1190307-88-0

Selleck's Sofosbuvir (GS-7977) has been cited by 34 publications

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DNA/RNA Synthesis Signaling Pathway Map

Biological Activity

Description

Sofosbuvir (PSI-7977, GS-7977) 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 Research:^[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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	529.45
Formula	C₂₂H₂₉FN₃O₉P
CAS No.	1190307-88-0
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
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

Download Sofosbuvir (GS-7977) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05140941	Not yet recruiting	Drug: Sofosbuvir/Velpatasvir 400 MG-100 MG Oral Tablet	Hepatitis C Chronic\|Pregnancy; Infection	Catherine Chappell\|Gilead Sciences\|University of Pittsburgh	February 1 2022	Phase 4
NCT04852614	Recruiting	Diagnostic Test: Pharmacokinetic test	Hepatitis C Virus Infection	Ain Shams University	December 1 2020	--
NCT04773756	Completed	Drug: Sofosbuvir 400 MG/ Daclatasvir 60mg	Covid19	Alexandria University	November 1 2020	Phase 4
NCT04382404	Recruiting	Drug: Sofosbuvir-Velpatasvir Drug Combination	Hepatitis C Chronic	Catherine Chappell\|Gilead Sciences\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|University of Pittsburgh	October 22 2020	Phase 1
NCT03903185	Unknown status	Drug: Ledipasvir / Sofosbuvir Oral Product	Hepatitis C Chronic\|Hematologic Malignancy	Ain Shams University\|Cairo University	March 1 2019	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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.

Handling Instructions

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