Referencia número: HY-12530

Velpatasvir

(Synonyms: GS-5816)

10 Cited Publications

Revisión del cliente

Based on 10 publication(s) in Google Scholar

Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 2.16 μM.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.83%
No. CAS: 1377049-84-7
Fòrmula: C₄₉H₅₄N₈O₈
Peso molecular:883.00

Almacenamiento:

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

Velpatasvir Chemical Structure

No. CAS: 1377049-84-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vivo
- Ensayo clínico
Chemical Information
Publications (10)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human HepG2 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human HepG2 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
HepG2	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human HepG2 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human HepG2 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
Huh-7	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human HuH7 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human HuH7 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
Huh-7	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human HuH7 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human HuH7 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
MRC5	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human MRC5 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human MRC5 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
MRC5	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human MRC5 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human MRC5 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
MT4	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human MT4 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human MT4 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
MT4	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human MT4 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human MT4 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
PC-3	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human PC3 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human PC3 cells infected with HCV genotype 1a H77 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]
PC-3	CC₅₀	>44400 nM Compound: 39; VEL, GS-5816	Cytotoxicity against human PC3 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay Cytotoxicity against human PC3 cells infected with HCV genotype 1b Con-1 assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo luminescent assay	[PMID: 31230974]

In Vivo

Velpatasvir (10 mg/kg/d, p.o.) alone or in combination with Sofosbuvir (HY-15005) (20 mg/kg/d) inhibits liver fibrosis in the CCl₄-induced non-HCV rat model^[3].

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

Animal Model:

CCl₄-induced non-HCV rat model^[3]
Dosage:

10 mg/kg/d alone, or in combination with Sofosbuvir (20 mg/kg/d)
Administration:

p.o.
Result:

Decreased the levels of TNF-a, NF-κB and IL-6 in serum and hepatic tissues.
Inhibited hepatic stellate cells (HSCs).

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1377049-84-7
Appearance Solid
Peso molecular 883.00
Fòrmula C₄₉H₅₄N₈O₈
Color White to off-white
SMILES

O=C(N([C@H]1C)[C@@H](CC1)C2=NC3=C(C(C=C(OCC4=CC(C5=CN=C([C@H](C[C@H](COC)C6)N6C([C@@H](C7=CC=CC=C7)NC(OC)=O)=O)N5)=CC=C84)C8=C9)=C9C=C3)N2)[C@H](C(C)C)NC(OC)=O
Synonyms

GS-5816
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (10)

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Journal Impact Factor

Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Hepatology

Resistance analysis of genotype 3 hepatitis C virus indicates subtypes inherently resistant to nonstructural protein 5A inhibitors. [Abstract]

2019 May;69(5):1861-1872. PMID: 29425396
Pharmaceuticals (Basel)

Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. [Abstract]

2022 Feb 18;15(2):242. PMID: 35215354
J Gastroenterol

Combinations of two drugs among NS3/4A inhibitors, NS5B inhibitors and non-selective antiviral agents are effective for hepatitis C virus with NS5A-P32 deletion in humanized-liver mice. [Abstract]

2019 May;54(5):449-458. PMID: 30684016
Sci Rep

Impact of novel NS5A resistance-associated substitutions of hepatitis C virus detected in treatment-experienced patients. [Abstract]

2019 Apr 5;9(1):5722. PMID: 30952914
Viruses

Resistance Analysis of a 3-Day Monotherapy Study with Glecaprevir or Pibrentasvir in Patients with Chronic Hepatitis C Virus Genotype 1 Infection. [Abstract]

2018 Aug 28;10(9). pii: E462. PMID: 30154359
Hepatol Res

Effects of resistance-associated variants in genotype 2 hepatitis C virus on viral replication and susceptibility to antihepatitis C virus drugs. [Abstract]

2019 Nov;49(11):1275-1285. PMID: 31261439
PLoS One

The combination of the NS5A and cyclophilin inhibitors results in an additive anti-HCV inhibition in humanized mice without development of resistance. [Abstract]

2021 May 20;16(5):e0251934. PMID: 34014993
J Chromatogr B Analyt Technol Biomed Life Sci

Quantification of second generation direct-acting antivirals daclatasvir, elbasvir, grazoprevir, ledipasvir, simeprevir, sofosbuvir and velpatasvir in human plasma by UPLC-MS/MS. [Abstract]

2019 Mar 15:1110-1111:15-24. PMID: 30776611
bioRxiv

The Cyclophilin Inhibitor Rencofilstat Decreases HCV-induced Hepatocellular Carcinoma Independently of Its Antiviral Activity. [Abstract]

2023 Aug 20:2023.08.19.553982. PMID: 37645728

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (113.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1325 mL

5.6625 mL

11.3250 mL

5 mM

0.2265 mL

1.1325 mL

2.2650 mL

10 mM

0.1133 mL

0.5663 mL

1.1325 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (2.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Lawitz EJ et al. Clinical Resistance to Velpatasvir (GS-5816), a Novel Pan-Genotypic Inhibitor of the Hepatitis C Virus NS5A Protein. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5368-78. [Content Brief]

[2]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

[3]. Yasmeen S, et al. An insight into the hepatoprotective role of Velpatasvir and Sofosbuvir per se and in combination against carbon tetrachloride-induced hepatic fibrosis in rats. Environ Sci Pollut Res Int. 2023 Sep;30(42):95660-95672. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1325 mL	5.6625 mL	11.3250 mL	28.3126 mL
	5 mM	0.2265 mL	1.1325 mL	2.2650 mL	5.6625 mL
	10 mM	0.1133 mL	0.5663 mL	1.1325 mL	2.8313 mL
	15 mM	0.0755 mL	0.3775 mL	0.7550 mL	1.8875 mL
	20 mM	0.0566 mL	0.2831 mL	0.5663 mL	1.4156 mL
	25 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1325 mL
	30 mM	0.0378 mL	0.1888 mL	0.3775 mL	0.9438 mL
	40 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
	50 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5663 mL
	60 mM	0.0189 mL	0.0944 mL	0.1888 mL	0.4719 mL
	80 mM	0.0142 mL	0.0708 mL	0.1416 mL	0.3539 mL
	100 mM	0.0113 mL	0.0566 mL	0.1133 mL	0.2831 mL

Keywords

Velpatasvir

10 Cited Publications

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Velpatasvir

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Velpatasvir

Actividad biológica

Chemical Information

Publications (10)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Velpatasvir

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Velpatasvir

Actividad biológica

Chemical Information

Publications (10)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Velpatasvir Related Classifications

HY-12530 Related Classifications