Art. -Nr.: HY-15602

Ledipasvir

(Synonyms: GS-5885)

31 Cited Publications

Kundenbewertung

Based on 31 publication(s) in Google Scholar

Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC₅₀s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.62 μM.

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Reinheit: 99.69%
CAS. Nr.: 1256388-51-8
Formel: C₄₉H₅₄F₂N₈O₆
Molecular Weight:889.00

Speicherung:

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

Ledipasvir Chemical Structure

CAS. Nr.: 1256388-51-8

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (31)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 34 pM (GT1a), 4 pM (GT1b)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	EC₅₀	210 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA	[PMID: 24320933]
Huh-7	EC₅₀	210 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum	[PMID: 24320933]
Huh-7	EC₅₀	27 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of 10% BSA	[PMID: 24320933]
Huh-7	EC₅₀	27 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay in presence of human serum	[PMID: 24320933]
Huh-7	EC₅₀	31 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay	[PMID: 24320933]
Huh-7	EC₅₀	4 pM Compound: 39, GS-5885, ledipasvir	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay	[PMID: 24320933]

In Vitro

Ledipasvir has GT1a and 1b EC₅₀ values of 31 and 4 pM, respectively, and protein-adjusted EC₅₀ values of 210 pM (GT1a) and 27 pM (GT1b) and the intrinsic EC₅₀ of 39 is 310 fM for GT1a and 40 fM for GT1b. Ledipasvir is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay^[1]. Ledipasvir exhibits an EC₅₀ value of 141 nM against the JFH/3a-NS5A replicon^[2].

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

In Vivo

Ledipasvir is remarkable not only on the basis of its high replicon potency but also on the basis of its low clearance, good bioavailability, and long half-lives in rat, dog, and monkey and low predicted clearance in human. The pharmacokinetics of Ledipasvir is measured in rats and dogs. Ledipasvir shows good half-lives (rat 1.83 ± 0.22 hr, dog 2.63 ± 0.18 hr) in plasma, low systemic clearance (CL), and moderate volumes of distribution (Vss) that are greater than total body water volume^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1256388-51-8
Appearance Solid
Molecular Weight 889.00
Formel C₄₉H₅₄F₂N₈O₆
Color Light yellow to yellow
SMILES

O=C(OC)N[C@H](C(N([C@H](C1=NC=C(C2=CC(C(F)(F)C3=C4C=CC(C5=CC=C6N=C([C@H]7N(C([C@@H](NC(OC)=O)C(C)C)=O)[C@]8([H])CC[C@@]7([H])C8)NC6=C5)=C3)=C4C=C2)N1)C9)CC%109CC%10)=O)C(C)C
Synonyms

GS-5885
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (31)

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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
Lancet Microbe

Hepatitis C virus diversity and treatment outcomes in Benin: a prospective cohort study. [Abstract]

2024 Jun 15:S2666-5247(24)00041-7. PMID: 38889738
Proc Natl Acad Sci U S A

Quantifying antiviral activity optimizes drug combinations against hepatitis C virus infection. [Abstract]

2017 Feb 21;114(8):1922-1927. PMID: 28174263
J Transl Med

Single-cell profiling of SLC family transporters: uncovering the role of SLC7A1 in osteosarcoma. [Abstract]

2025 Jan 22;23(1):103. PMID: 39844299
Biomed Pharmacother

FDA-approved antivirals ledipasvir and daclatasvir downregulate the Src-EPHA2-Akt oncogenic pathway in colorectal and triple-negative breast cancer cells. [Abstract]

2024 Sep 2:179:117325. PMID: 39226729
Int J Radiat Oncol Biol Phys

Targeting Phosphatidylinositol 4-Kinase IIIα for Radiosensitization: A Potential Model of Drug Repositioning Using an Anti-Hepatitis C Viral Agent. [Abstract]

2016 Nov 15;96(4):867-876. PMID: 27788957
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
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
Antimicrob Agents Chemother

Fast hepatitis C virus RNA elimination and NS5A redistribution by NS5A inhibitors studied by a multiplex assay approach. [Abstract]

2015;59(6):3482-92. PMID: 25845863

Ledipasvir purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2015;59(6):3482-92. [Abstract]

Assessment of HCV inhibition by DAAs from 3 classes using Western blot analysis. Jc1/Gluc2A virus-infected Huh-7.5.1 cells are treated with DMSO or the HCV inhibitors at concentrations of 100× EC₅₀ (DCV, 3.2 nM; LDV, 3 μM; DNV, 0.32 μM; SOF, 20 μM). Cell lysates are harvested at 8 hpt (C and D) or at 24 hpt (A and B) and blotted for NS5A (A and C) or core (B and D). Data are normalized to GAPDH and quantified as relative fold change with respect to DMSO.
Antimicrob Agents Chemother

Cyclophilin and NS5A inhibitors, but not other anti-hepatitis C virus (HCV) agents, preclude HCV-mediated formation of double-membrane-vesicle viral factories. [Abstract]

2015 May;59(5):2496-507. PMID: 25666154
Antimicrob Agents Chemother

Hepatitis C virus genotype 5a subgenomic replicons for evaluation of direct-acting antiviral agents. [Abstract]

2014 Sep;58(9):5386-94. PMID: 24982066
Ann Hepatol

Sofosbuvir inhibits yellow fever virus in vitro and in patients with acute liver failure. [Abstract]

Nov-Dec 2019;18(6):816-824. PMID: 31594756
Drug Metab Dispos

A Systematic In Vitro Investigation of the Inhibitor Preincubation Effect on Multiple Classes of Clinically Relevant Transporters. [Abstract]

2019 Jul;47(7):768-778. PMID: 31068368
Antiviral Res

A profiling study of a newly developed HCVcc strain PR63cc's sensitivity to direct-acting antivirals. [Abstract]

2017 Mar;139:18-24. PMID: 28025084
Viruses

Mechanisms of Action of the Host-Targeting Agent Cyclosporin A and Direct-Acting Antiviral Agents against Hepatitis C Virus. [Abstract]

2023 Apr 17;15(4):981. PMID: 37112961
Viruses

Visualization of Positive and Negative Sense Viral RNA for Probing the Mechanism of Direct-Acting Antivirals against Hepatitis C Virus. [Abstract]

2019 Nov 8;11(11):1039. PMID: 31717338
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
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
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
Transpl Infect Dis

The influence of immunosuppressants on direct-acting antiviral therapy is dependent on the hepatitis C virus genotype. [Abstract]

2018 Feb;20(1). PMID: 29111569
PLoS One

Cyclophilin Inhibitors Remodel the Endoplasmic Reticulum of HCV-Infected Cells in a Unique Pattern Rendering Cells Impervious to a Reinfection. [Abstract]

2016 Jul 21;11(7):e0159511. PMID: 27442520
Neurosci Lett

Critical role of Casein kinase 2 in hepatitis C NS5A-mediated inhibition of Kv2.1 K(+) channel function. [Abstract]

2015 Nov 16;609:48-52. PMID: 26472706
Biomed Chromatogr

In-depth investigation of the Silymarin effect on the pharmacokinetic parameters of sofosbuvir, GS-331007 and ledipasvir in rat plasma using LC-MS. [Abstract]

2022 Sep;36(9):e5427. PMID: 35708053
University of Glasgow

2024 Mar.
University of Colorado Denver

2024.
F1000Res

2019 Oct.
University Estadual De Campinas Institudo De Biologia

2019 Sep.
bioRxiv

2019 Aug.
Charles University

2019 Jun.
Seoul National University

2016 Aug.
North-West University

2014 Oct.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (56.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.1249 mL

5.6243 mL

11.2486 mL

5 mM

0.2250 mL

1.1249 mL

2.2497 mL

10 mM

0.1125 mL

0.5624 mL

1.1249 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (2.81 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.81 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

Protokoll

Animal Administration^[1]

Rats, Dogs and Monkeys^[1]
Pharmacokinetic studies are performed in male naı̈ve Sprague-Dawley(SD) rats, non-naive beagle dogs, and cynomolgus monkeys (three animals per dosing route). Intravenous (IV) administration is dosed via infusion over 30 min in a vehicle containing 5% ethanol, 20% PEG400, and 75% water (pH adjusted to 3.0 with HCl). Oral dosing is administered by gavage in a vehicle containing 5% ethanol, 45% PEG 400, and 50% of 50 mM citrate buffer, pH 3. Blood samples are collected over a 24 h period postdose into Vacutainer tubes containing EDTA-K2. Plasma was isolated, and the concentration of the test compound in plasma was determined with LC/MS/MS after protein precipitation with acetonitrile.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)
- 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)
Handling Instructions (2659 KB)

Verweise

[1]. Link JO, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46 [Content Brief]

[2]. Hernandez D, et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013 May;57(1):13-8. [Content Brief]

[3]. 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]

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	1.1249 mL	5.6243 mL	11.2486 mL	28.1215 mL
	5 mM	0.2250 mL	1.1249 mL	2.2497 mL	5.6243 mL
	10 mM	0.1125 mL	0.5624 mL	1.1249 mL	2.8121 mL
	15 mM	0.0750 mL	0.3750 mL	0.7499 mL	1.8748 mL
	20 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4061 mL
	25 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1249 mL
	30 mM	0.0375 mL	0.1875 mL	0.3750 mL	0.9374 mL
	40 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7030 mL
	50 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5624 mL

Keywords

Ledipasvir

31 Cited Publications

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Ledipasvir

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Rare Diseases Drug Library

Pediatric Drug 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

Publications Citing Use of MedChemExpress (MCE) Ledipasvir

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ledipasvir

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Rare Diseases Drug Library

Pediatric Drug 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

Publications Citing Use of MedChemExpress (MCE) Ledipasvir

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ledipasvir Related Classifications

Art. -Nr.: HY-15602