Sofosbuvir (Synonyms: GS-7977; PSI-7977)

Name: Sofosbuvir
Brand: MedChemExpress
SKU: HY-15005
Rating: 5.0 (106 reviews)

Cat. No.: HY-15005 Purity: 99.97%: FAQs
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Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC₅₀ of 92 nM.

For research use only. We do not sell to patients.

Sofosbuvir Chemical Structure

CAS No. : 1190307-88-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 106 publication(s) in Google Scholar

Other Forms of Sofosbuvir:

102 Publications Citing Use of MCE Sofosbuvir

: Sofosbuvir purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065. [Abstract]; GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), Sofosbuvir (0.8 μM), Daclatasvir (0.15 μM) or solvent control for 6 days.

: Sofosbuvir purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065. [Abstract]; Huh7.5 cells are infected with HCV and simultaneously treated with 7f (10 μM) or DAA (0.04 μM Simeprevir, 0.08 μM Sofosbuvir, or 16 pM Daclatasvir) or 7f plus DAA.

: Sofosbuvir purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2017;2017:1236801. [Abstract]; Huh7.5 (HCV+) cells are treated with 1 μM of Sofosbuvir or solvent control. At 24 hours, the cells are washed and continuously incubated with fresh culture media containing drugs again for 48 hours. The cultural supernatants are then harvested and directly incubated to naïve Huh7.5 cells. After been passaged 1~3 times, the newly infected cells are treated with 1 μM of Sofosbuvir for 72 hours. Intracellular proteins are extracted and detected with WB.

: Sofosbuvir purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Nov 23;59(22):10268-10284. [Abstract]; Huh7.5 cells are infected with HCV (45 IU/cell) and simultaneously treated with Simeprevir (A, 0.025 μM), Sofosbuvir (B, 0.1 μM), or Daclatasvir (C, 16 pM) alone or with 1 (6.25 μM).

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC₅₀ of 92 nM^[1].

IC₅₀ & Target

EC50: 92±5 nM (HCV)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Cardiac muscle cell	CC₅₀	> 300 μM Compound: SOF	Cardiotoxicity against human embryonic stem cell-induced ventricular cardiomyocytes administered on day 7 and measured on day 10 after 30 mins incubation by CellTiter Glo assay Cardiotoxicity against human embryonic stem cell-induced ventricular cardiomyocytes administered on day 7 and measured on day 10 after 30 mins incubation by CellTiter Glo assay	[PMID: 30653317]
CCRF-CEM	CC₅₀	> 100 μM Compound: SOF	Cytotoxicity against human CCRF-CEM assessed reduction in cell viability after 4 days by MTT assay Cytotoxicity against human CCRF-CEM assessed reduction in cell viability after 4 days by MTT assay	[PMID: 30653317]
CCRF-CEM	CC₅₀	> 100 μM Compound: 1; SOF	Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 4 days by MTT assay Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 4 days by MTT assay	[PMID: 28595015]
CCRF-CEM	CC₅₀	> 100 μM Compound: Sofosbuvir	Cytotoxicity against human CEM cells assessed as reduction in cell viability after 6 days by trypan blue exclusion assay Cytotoxicity against human CEM cells assessed as reduction in cell viability after 6 days by trypan blue exclusion assay	[PMID: 29066308]
CCRF-CEM	CC₅₀	> 100 μM Compound: SOF; 1	Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion method Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion method	[PMID: 30655167]
HepaRG	CC₅₀	44 μM Compound: SOF	Cytotoxicity in human HepaRG cells assessed as reduction in cell viability incubated for 14 days by CellTiter-Glo assay Cytotoxicity in human HepaRG cells assessed as reduction in cell viability incubated for 14 days by CellTiter-Glo assay	[PMID: 30653317]
Hepatocyte	CC₅₀	> 300 μM Compound: SOF	Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30653317]
HepG2	CC₅₀	> 50 μM Compound: Sofosbuvir	Cytotoxicity against human HepG2 cells after 96 hrs by CCK-8 assay Cytotoxicity against human HepG2 cells after 96 hrs by CCK-8 assay	[PMID: 29801997]
HepG2	IC₅₀	> 50 μM Compound: 1; SOF	Mitochondrial toxicity in human HepG2 cells assessed as inhibition of cytochrome c oxidase subunit 2 DNA levels measured on day 14 by RT-PCR method Mitochondrial toxicity in human HepG2 cells assessed as inhibition of cytochrome c oxidase subunit 2 DNA levels measured on day 14 by RT-PCR method	[PMID: 28595015]
HepG2	IC₅₀	> 50 μM Compound: 1; SOF	Cytotoxicity against human HepG2 cells assessed as inhibition of nuclear DNA levels measured on day 14 by RT-PCR method Cytotoxicity against human HepG2 cells assessed as inhibition of nuclear DNA levels measured on day 14 by RT-PCR method	[PMID: 28595015]
HepG2	IC₅₀	> 50 μM Compound: SOF	Mitochondrial toxicity in human HepG2 cells assessed as inhibition of cytochrome c oxidase subunit 2 DNA level followed by medium plus drugs replenishment every 3 to 4 days for 14 days relative to control Mitochondrial toxicity in human HepG2 cells assessed as inhibition of cytochrome c oxidase subunit 2 DNA level followed by medium plus drugs replenishment every 3 to 4 days for 14 days relative to control	[PMID: 30653317]
HepG2	IC₅₀	45 μM Compound: SOF	Mitochondrial toxicity in human HepG2 cells assessed as inhibition of nuclear ribosomal-DNA level followed by medium plus drugs replenishment every 3 to 4 days for 14 days relative to control Mitochondrial toxicity in human HepG2 cells assessed as inhibition of nuclear ribosomal-DNA level followed by medium plus drugs replenishment every 3 to 4 days for 14 days relative to control	[PMID: 30653317]
HK-2	CC₅₀	> 300 μM Compound: SOF	Nephrotoxicity in human HK2 cells after 72 hrs by Hoechst 33342/HCS live/dead green dye-based assay Nephrotoxicity in human HK2 cells after 72 hrs by Hoechst 33342/HCS live/dead green dye-based assay	[PMID: 30653317]
Huh-7	CC₅₀	> 10 μM Compound: 1; SOF	Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 4 days by MTS assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 4 days by MTS assay	[PMID: 28595015]
Huh-7	CC₅₀	> 10 μM Compound: Sofosbuvir	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability by MTT assay	[PMID: 29066308]
Huh-7	CC₅₀	> 100 μM Compound: SOF	Cytotoxicity against human HuH7 cells assessed reduction in cell viability after 3 to 5 days by MTT assay Cytotoxicity against human HuH7 cells assessed reduction in cell viability after 3 to 5 days by MTT assay	[PMID: 30653317]
Huh-7	CC₅₀	> 100 μM Compound: SOF; 1	Cytotoxicity against human HuH7 cells assessed as reduction in rRNA levels after 5 days by RT-PCR analysis Cytotoxicity against human HuH7 cells assessed as reduction in rRNA levels after 5 days by RT-PCR analysis	[PMID: 30655167]
Huh-7	CC₅₀	> 100 μM Compound: PSI-7977	Cytotoxicity against human Huh7.5.1 cells after 48 hrs by luciferase reporter gene assay Cytotoxicity against human Huh7.5.1 cells after 48 hrs by luciferase reporter gene assay	[PMID: 27994763]
Huh-7	CC₅₀	> 1000 μM Compound: 17	Cytotoxicity against human HuH7 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human HuH7 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 29172078]
Huh-7	CC₅₀	> 20 μM Compound: Sofosbuvir	Cytotoxicity against human HuH7 cells infected with HCV genotype 1b replicon after 72 hrs by CellTiter-Fluor reagent based fluorescence assay Cytotoxicity against human HuH7 cells infected with HCV genotype 1b replicon after 72 hrs by CellTiter-Fluor reagent based fluorescence assay	[PMID: 30683552]
Huh-7	EC₅₀	0.053 μM Compound: 1	Antiviral activity against HCV genotype 1b Con1 over expressing CES1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b Con1 over expressing CES1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay	[PMID: 31740203]
Huh-7	EC₅₀	0.062 μM Compound: 1	Antiviral activity against HCV genotype 1b Con1 expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 1b Con1 expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.0751 μM Compound: 1	Antiviral activity against HCV genotype 3a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 3a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.0785 μM Compound: 1	Antiviral activity against HCV genotype 4a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 4a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.0867 μM Compound: 1	Antiviral activity against HCV genotype 6a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 6a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.12 μM Compound: PSI-7977	Antiviral activity against HCV JFH-1 infected in human HuH7.5.1 cells after 48 hrs by luciferase reporter gene assay Antiviral activity against HCV JFH-1 infected in human HuH7.5.1 cells after 48 hrs by luciferase reporter gene assay	[PMID: 27994763]
Huh-7	EC₅₀	0.155 μM Compound: Sofosbuvir	Inhibition of NS5B polymerase in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay Inhibition of NS5B polymerase in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay	[PMID: 32046903]
Huh-7	EC₅₀	0.155 μM Compound: 1	Antiviral activity against HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay	[PMID: 31740203]
Huh-7	EC₅₀	0.188 μM Compound: 1	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay	[PMID: 31740203]
Huh-7	EC₅₀	0.23 μM Compound: Sofosbuvir	Inhibition of NS5B polymerase in HCV genotype 1b Con1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay Inhibition of NS5B polymerase in HCV genotype 1b Con1 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay	[PMID: 32046903]
Huh-7	EC₅₀	0.254 μM Compound: 25	Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay	[PMID: 24345201]
Huh-7	EC₅₀	0.3301 μM Compound: 1	Antiviral activity against HCV genotype 3a expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 3a expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.6376 μM Compound: 1	Antiviral activity against HCV genotype 1b Con1 expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 1b Con1 expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	0.6813 μM Compound: 1	Antiviral activity against HCV genotype 2a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 2a expressing wild type NS5B infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	EC₅₀	1.002 μM Compound: 1	Antiviral activity against HCV genotype 2a expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay Antiviral activity against HCV genotype 2a expressing NS5B S282T mutant infected in human HuH7 replicon cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene based assay	[PMID: 31740203]
Huh-7	CC₅₀	200 μM Compound: Sofosbuvir	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability by measuring ATP level measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability by measuring ATP level measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 32435411]
Huh-7	CC₅₀	200 μM Compound: Sofosbuvir	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by Celltiter-Glo luminescent cell viability assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by Celltiter-Glo luminescent cell viability assay	[PMID: 34273661]
Huh-7	IC₅₀	3.8 μM Compound: Sofosbuvir	Antiviral activity against Dengue virus serotype 2 New Guinea C infected at 50 TCID50 in human HuH7 cells assessed as inhibition of viral replication and 72 hrs later re-infected pre-seeded HuH7 cells with viral supernatant collected from previous infecte Antiviral activity against Dengue virus serotype 2 New Guinea C infected at 50 TCID50 in human HuH7 cells assessed as inhibition of viral replication and 72 hrs later re-infected pre-seeded HuH7 cells with viral supernatant collected from previous infecte	[PMID: 32435411]
Huh-7.5	CC₅₀	> 200 μM Compound: SOF	Cytotoxicity against human Huh7.5 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human Huh7.5 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 35050619]
Huh-7.5	CC₅₀	121.47 μM Compound: SOF	Cytotoxicity against human Huh7.5 cells carrying HCV subgenomic replicons assessed as reduction in cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human Huh7.5 cells carrying HCV subgenomic replicons assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 35050619]
Huh-7.5	CC₅₀	170.85 μM Compound: SOF	Cytotoxicity against human Huh7.5 cells infected with HCVcc assessed as reduction in cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human Huh7.5 cells infected with HCVcc assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 35050619]
PBMC	CC₅₀	> 100 μM Compound: SOF	Cytotoxicity against human PBMC assessed reduction in cell viability after 5 days by MTT assay Cytotoxicity against human PBMC assessed reduction in cell viability after 5 days by MTT assay	[PMID: 30653317]
PBMC	CC₅₀	> 100 μM Compound: 1; SOF	Cytotoxicity against human PBMC assessed as inhibition of cell proliferation after 5 days by MTT assay Cytotoxicity against human PBMC assessed as inhibition of cell proliferation after 5 days by MTT assay	[PMID: 28595015]
PBMC	CC₅₀	> 100 μM Compound: Sofosbuvir	Cytotoxicity against human PBMC assessed as reduction in cell viability after 6 days by trypan blue exclusion assay Cytotoxicity against human PBMC assessed as reduction in cell viability after 6 days by trypan blue exclusion assay	[PMID: 29066308]
PBMC	CC₅₀	> 100 μM Compound: SOF; 1	Cytotoxicity against human PBMC after 6 days by trypan blue exclusion method Cytotoxicity against human PBMC after 6 days by trypan blue exclusion method	[PMID: 30655167]
Vero	CC₅₀	> 100 μM Compound: SOF	Cytotoxicity against African green monkey Vero cells assessed reduction in cell viability after 3 days by MTT assay Cytotoxicity against African green monkey Vero cells assessed reduction in cell viability after 3 days by MTT assay	[PMID: 30653317]
Vero	CC₅₀	> 100 μM Compound: 1; SOF	Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell proliferation after 3 days by MTT assay Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell proliferation after 3 days by MTT assay	[PMID: 28595015]
Vero	CC₅₀	> 100 μM Compound: Sofosbuvir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 6 days by trypan blue exclusion assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 6 days by trypan blue exclusion assay	[PMID: 29066308]
Vero	CC₅₀	> 100 μM Compound: SOF; 1	Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometric method Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometric method	[PMID: 30655167]
Vero	EC₅₀	30.9 μM Compound: 5	Inhibition of RNA-dependent RNA polymerase in Zika virus infected in African green monkey Vero cells assessed as antiviral activity by DAPI-staining based assay Inhibition of RNA-dependent RNA polymerase in Zika virus infected in African green monkey Vero cells assessed as antiviral activity by DAPI-staining based assay	[PMID: 31549836]

In Vitro

When cathepsin A (CatA) is incubated with PSI-7977 or Sofosbuvir (PSI-7977) for 150 min, ~18-fold more PSI-352707 is formed when Sofosbuvir (PSI-7977) is the substrate compared with PSI-7976. Moreover, the catalytic efficiency for Sofosbuvir (PSI-7977) with CatA is ~30-fold higher than that for PSI-7976^[1]. The genotype coverage of Sofosbuvir (PSI-7977) by using GT 1b (Con1)-, 1a (H77)-, and 2a (JFH-1)-derived replicons and GT 1b chimeric replicons containing the NS5B region from the J6 GT 2a isolate and from GT 2b and GT 3a patient isolates is evaluated, Sofosbuvir (PSI-7977) inhibits the replication of these replicons with similar EC₅₀s (between 16 and 48 nM), and is especially active against the chimeric replicon containing the J6 NS5B (EC₅₀=4.7 nM). Sofosbuvir (PSI-7977) inhibits clone A (GT 1b) wild-type and S282T replicons with EC₉₀ values of 0.42 and 7.8 μM, respectively^[2]. In the clone A replicon assay, Sofosbuvir (PSI-7977) produces anti-HCV activity with EC₉₀ values 0.42 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

529.45

Formula

C₂₂H₂₉FN₃O₉P

CAS No.

1190307-88-0

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1(F)[C@H](O)[C@@H](CO[P@](OC2=CC=CC=C2)(N[C@@H](C)C(OC(C)C)=O)=O)O[C@H]1N(C=CC(N3)=O)C3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (94.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (47.22 mM; ultrasonic and warming and heat to 50°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 4.55 mg/mL (8.59 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (257 KB) RP-HPLC (276 KB)

Handling Instructions (2659 KB)

References

[1]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47. [Content Brief]

[2]. Lam AM, et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68. [Content Brief]

[3]. Sofia MJ, et al. Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18. [Content Brief]

[4]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065. [Content Brief]

Cell Assay
^[1]

Clone A cells are seeded into T75 flasks at about 5×10⁶ cells/flask in Dulbecco's modified Eagle's medium (DMEM) containing 100 IU/mL Penicillin/100 μg/mL streptomycin and 10% fetal bovine serum. Similarly, human primary hepatocytes are seeded in cell plating medium into T75 flasks at about 5×10⁶ cells/flask. After overnight incubation to allow the cells to attach, 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 h at 37°C in a 5% CO₂ atmosphere. The same procedures are applied when radiolabeled PSI-7851 is used in the study except that 1×10⁶ cells per well are seeded into a 6-well plate, and the cells are incubated with 5 μM [³H]PSI-7851. At selected times, the medium is removed, and the cell layer is washed with cold phosphate-buffered saline (PBS). After trypsinization, cells are counted and centrifuged at 1,200 rpm for 5 min. The cell pellets are suspended in 1 mL of cold 60% methanol and incubated overnight at −20°C. The samples are centrifuged at 14,000 rpm for 5 min, and the supernatants are collected and dried using a SpeedVac concentrator and stored at −20°C until they are analyzed by high performance liquid chromatography (HPLC). Residues are suspended in 100 μL of water, and 50-μL aliquots are injected into HPLC^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47. [Content Brief]

[2]. Lam AM, et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68. [Content Brief]

[3]. Sofia MJ, et al. Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18. [Content Brief]

[4]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8888 mL	9.4438 mL	18.8875 mL	47.2188 mL
	5 mM	0.3778 mL	1.8888 mL	3.7775 mL	9.4438 mL
	10 mM	0.1889 mL	0.9444 mL	1.8888 mL	4.7219 mL
	15 mM	0.1259 mL	0.6296 mL	1.2592 mL	3.1479 mL
	20 mM	0.0944 mL	0.4722 mL	0.9444 mL	2.3609 mL
	25 mM	0.0756 mL	0.3778 mL	0.7555 mL	1.8888 mL
	30 mM	0.0630 mL	0.3148 mL	0.6296 mL	1.5740 mL
	40 mM	0.0472 mL	0.2361 mL	0.4722 mL	1.1805 mL
DMSO	50 mM	0.0378 mL	0.1889 mL	0.3778 mL	0.9444 mL
	60 mM	0.0315 mL	0.1574 mL	0.3148 mL	0.7870 mL
	80 mM	0.0236 mL	0.1180 mL	0.2361 mL	0.5902 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Sofosbuvir1190307-88-0GS-7977 PSI-7977GS7977GS 7977PSI7977PSI 7977PSI-7977HCVHepatitis C virusInhibitorinhibitorinhibit

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Sofosbuvir (Synonyms: GS-7977; PSI-7977)

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