Sofosbuvir (PSI-7977; GS-7977)

Alias: PSI-7977; GS7977; PSI 7977; GS-7977; PSI7977; GS 7977; Vosevi; Hepcinat; Hepcvir; Resof; Sofosbuvir; Sovaldi; Virunon

Cat No.:V1477 Purity: ≥98%

COA Product Data Instructions for use SDS

Sofosbuvir (PSI-7977; GS-7977) Chemical Structure CAS No.: 1190307-88-0
Product category: DNA(RNA) Synthesis

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Sofosbuvir (also known as PSI-7977, GS-7977; PSI7977; GS7977; Vosevi; Hepcinat; Hepcvir; Resof; Sovaldi and Virunon), a blockbuster anti-HCV drug, is an HCV NS5B polymerase inhibitor that has been approved for the treatment of chronic hepatitis C virus (HCV) infections. Sofosbuvir acts by blocking the hepatitis C virus from using RNA polymerase to replicate its RNA. It is a part of the first approved treatment regimen for chronic Hepatitis C that is all oral and devoid of interferon. The FDA approved sofosbuvir and ribavirin (RBV) in 2013 for treatment-naive patients with HCV genotypes 1 and 4. Additionally, patients with genotypes 2 and 3 were approved for triple therapy using injected pegylated interferon (pegIFN) and RBV.

Biological Activity I Assay Protocols (From Reference)

Targets

HCV ( EC50 = 92±5 nM )

ln Vitro

PSI-7977, an HCV NS5B polymerase inhibitor, exhibits a more potent inhibitory activity against HCV RNA replication than PSI-7976, as evidenced by its EC50 of 92 nM versus 1.07 μM and EC90 of 0.29 μM versus 2.99 μM. This is consistent with the finding that clone A cells incubated with PSI-7977 produce a higher concentration of PSI-7409 than clone A cells incubated with PSI-7976. By virtue of its 18–30 fold increase in potency over PSI–7976, PSI–7977 is a more effective substrate for CatA to form PSI–352707. However, unlike GS-7976, PSI-7977's CES1-mediated hydrolysis does not proceed in a time-dependent fashion.[1] Resistance to PSI-7977 can be conferred by the S282T NS5B polymerase mutation, but not by the S96T mutation. The EC90 value increases from 0.42 μM to 7.8 μM. Even at concentrations as high as 100 μM, PSI-7977 shows no cytotoxicity against Huh7, HepG2, BxPC3, and CEM cells in an 8-day cytotoxicity assay. After 14 days of treatment with PSI-7977, the inhibition of mtDNA and rDNA in HepG2 cells was shown to have an IC90 of 72.1 μM and 68.6 μM, respectively. [/2] With regard to genotype (GT) 1a, 1b, and 2a (strain JFH-1) replicons as well as chimeric replicons containing GT 2a (strain J6), 2b, and 3a NS5B polymerase, PSI-7977 demonstrates strong activity. Additional amino acid changes, such as T179A, M289L, I293L, M434T, and H479P, are chosen both before and after the emergence of S282T, which is necessary to confer resistance to PSI-7977, according to sequence analysis of the JFH-1 NS5B region.[3]

ln Vivo

The average plasma ALT levels in the 440- and 44-mg/kg/d treatment groups of mice with humanized livers were below the upper limit of normal and did not differ statistically from those in the vehicle-treated humanized liver mice. Additionally, neither the control mice nor the mice with humanized livers that received either dose of PSI-7977 had elevated plasma lactate levels.

Cell Assay

In T75 flasks, clone A cells are deposited at a density of approximately 5×10⁶ cells/flask using Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 IU/mL Penicillin, and 100 μg/mL streptomycin. In a similar manner, T75 flasks are seeded with approximately 5×10⁶ human primary hepatocytes per flask using cell plating medium. Cells are incubated with 50 μM PSI-7851, PSI-7976, or Sofosbuvir (PSI-7977) in fresh medium for clone A cells or in cell maintenance medium for primary hepatocytes for up to 24 hours at 37°C in a 5% CO₂ atmosphere after being left to attach overnight. When using radiolabeled PSI-7851 in the study, the same protocols are followed, with the exception that 1×10⁶ cells are seeded into each well of a 6-well plate, and the cells are then incubated with 5 μM [³H]PSI-7851. The medium is taken out at predetermined intervals, and the cell layer is cleaned using cold phosphate-buffered saline (PBS). Following trypsinization, cells are tallied and centrifuged for five minutes at 1,200 rpm. The cell pellets are left overnight at −20°C after being suspended in 1 mL of cold 60% methanol. After centrifuging the samples for five minutes at 14,000 rpm, the supernatants are gathered, dried with a SpeedVac concentrator, and kept at -20°C until high performance liquid chromatography (HPLC) analysis. After suspending residues in 100 μL of water, 50 μL aliquots are injected into an HPLC.

Animal Protocol

Oral administration, 44 or 440 mg/kg

TK-NOG mice with non-humanized (control) or humanized livers

References

[1]. J Biol Chem . 2010 Nov 5;285(45):34337-47.

[2]. J Med Chem . 2010 Oct 14;53(19):7202-18.

[3]. Antimicrob Agents Chemother . 2012 Jun;56(6):3359-68.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C22H29FN3O9P

Molecular Weight

529.45

Exact Mass

529.16

Elemental Analysis

C, 49.91; H, 5.52; F, 3.59; N, 7.94; O, 27.20; P, 5.85

CAS #

1190307-88-0

Related CAS #

1190307-88-0

Appearance

White solid powder

SMILES

C[C@@H](C(=O)OC(C)C)N[P@](=O)(OC[C@@H]1[C@H]([C@@]([C@@H](O1)N2C=CC(=O)NC2=O)(C)F)O)OC3=CC=CC=C3

InChi Key

TTZHDVOVKQGIBA-IQWMDFIBSA-N

InChi Code

InChI=1S/C22H29FN3O9P/c1-13(2)33-19(29)14(3)25-36(31,35-15-8-6-5-7-9-15)32-12-16-18(28)22(4,23)20(34-16)26-11-10-17(27)24-21(26)30/h5-11,13-14,16,18,20,28H,12H2,1-4H3,(H,25,31)(H,24,27,30)/t14-,16+,18+,20+,22+,36-/m0/s1

Chemical Name

propan-2-yl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate

Synonyms

PSI-7977; GS7977; PSI 7977; GS-7977; PSI7977; GS 7977; Vosevi; Hepcinat; Hepcvir; Resof; Sofosbuvir; Sovaldi; Virunon

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 50~100 mg/mL (94.4~188.9 mM)

Water: ~11 mg/mL (~20.8mM)

Ethanol: ~100 mg/mL (~188.9 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.8888 mL	9.4438 mL	18.8875 mL
	5 mM	0.3778 mL	1.8888 mL	3.7775 mL
	10 mM	0.1889 mL	0.9444 mL	1.8888 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

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

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03855917	Recruiting	Drug: Sofosbuvir 400mg [Sovaldi] Drug: Glecaprevir/pibrentasvir (300mg/120mg)	Hepatitis C	Kirby Institute	February 11, 2020	Phase 4
NCT03540212	Recruiting	Drug: Daclatasvir and sofosbuvir	Chronic HCV Infection	Ain Shams University	January 2009	Phase 2 Phase 3
NCT03646396	Recruiting	Drug: Sofosbuvir-daclatasvir	HCV Coinfection	Sherief Abd-Elsalam	August 1, 2018	Not Applicable
NCT05854511	Recruiting	Drug: Sofosbuvir 200 MG Oral Tablet plus Daclatasvir 30 mg Oral tablets	HCV	Ain Shams University	June 5, 2022	Phase 3
NCT04852614	Recruiting	Diagnostic Test: Pharmacokinetic test	Hepatitis C Virus Infection	Ain Shams University	December 1, 2020	N/A

Biological Data

Locations of the PSI-7977-selected amino acid changes using JFH-1 NS5B (Protein Data Bank accession number 3I5K). Antimicrob Agents Chemother . 2012 Jun;56(6):3359-68.