Sofosbuvir (PSI-7977, GS-7977)

Catalog No.S2794

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

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Sofosbuvir (PSI-7977, GS-7977) Chemical Structure

Sofosbuvir (PSI-7977, GS-7977) Chemical Structure
Molecular Weight: 529.45

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
In vivo
Features

Protocol(Only for 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Murakami E, et al. J Biol Chem, 2010, 285(45), 34337-34347.

[2] Sofia MJ, et al. J Med Chem, 2010, 53(19), 7202-7218.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02631772 Not yet recruiting Hepatitis C Medical University of South Carolina June 2016 Phase 4
NCT02772744 Not yet recruiting Hepatitis C Zagazig University|Cairo University June 2016 --
NCT02781649 Not yet recruiting End-Stage Renal Disease|Hepatitis C Johns Hopkins University|Merck Sharp & Dohme Corp. June 2016 Phase 1
NCT02705534 Not yet recruiting Hepatitis C|Cirrhosis Tehran University of Medical Sciences|Bakhtar Bioshimi Co April 2016 Phase 3
NCT02683005 Not yet recruiting Hepatitis C|Pregnancy University of Pittsburgh|Gilead Sciences|University of Ne  ...more University of Pittsburgh|Gilead Sciences|University of Nebraska April 2016 Phase 1

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Chemical Information

Download Sofosbuvir (PSI-7977, GS-7977) SDF
Molecular Weight (MW) 529.45
Formula

C22H29FN3O9P

CAS No. 1190307-88-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL warmed (188.87 mM)
Ethanol 100 mg/mL (188.87 mM)
Water 11 mg/mL warmed (20.77 mM)
In vivo
* <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.
Chemical Name L-Alanine, N-[[P(S),2'R]-2'-deoxy-2'-fluoro-2'-methyl-P-phenyl-5'-uridylyl]-, 1-methylethyl ester

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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