Art. -Nr.: HY-15602A

Ledipasvir (acetone)

(Synonyms: GS-5885 (acetone))

31 Cited Publications

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Based on 31 publication(s) in Google Scholar

Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC₅₀ values of 34 pM against GT1a and 4 pM against GT1b replicon.

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Reinheit: 99.92%
CAS. Nr.: 1441674-54-9
Formel: C₅₂H₆₀F₂N₈O₇
Molecular Weight:947.08

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Ledipasvir (acetone) Chemical Structure

CAS. Nr.: 1441674-54-9

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

Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Publications (31)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Ledipasvir acetone is considered the active ingredient, which is converted to Ledipasvir spray-dried dispersion, an amorphous free base.

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

Chemical Information

CAS. Nr. 1441674-54-9
Appearance Solid
Molecular Weight 947.08
Formel C₅₂H₆₀F₂N₈O₇
Color Off-white 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.CC(C)=O
Synonyms

GS-5885 (acetone)
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 Jul;5(7):697-706. PMID: 38889738
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
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
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
Ann Hepatol

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

2019 Nov-Dec;18(6):816-824. PMID: 31594756
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
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
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 (acetone) 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
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):462. PMID: 30154359
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
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
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
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
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
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
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 Oct:179:117325. PMID: 39226729
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 : 100 mg/mL (105.59 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

1.0559 mL

5.2794 mL

10.5588 mL

5 mM

0.2112 mL

1.0559 mL

2.1118 mL

10 mM

0.1056 mL

0.5279 mL

1.0559 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (2.64 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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)
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]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0559 mL	5.2794 mL	10.5588 mL	26.3969 mL
	5 mM	0.2112 mL	1.0559 mL	2.1118 mL	5.2794 mL
	10 mM	0.1056 mL	0.5279 mL	1.0559 mL	2.6397 mL
	15 mM	0.0704 mL	0.3520 mL	0.7039 mL	1.7598 mL
	20 mM	0.0528 mL	0.2640 mL	0.5279 mL	1.3198 mL
	25 mM	0.0422 mL	0.2112 mL	0.4224 mL	1.0559 mL
	30 mM	0.0352 mL	0.1760 mL	0.3520 mL	0.8799 mL
	40 mM	0.0264 mL	0.1320 mL	0.2640 mL	0.6599 mL
	50 mM	0.0211 mL	0.1056 mL	0.2112 mL	0.5279 mL
	60 mM	0.0176 mL	0.0880 mL	0.1760 mL	0.4399 mL
	80 mM	0.0132 mL	0.0660 mL	0.1320 mL	0.3300 mL
	100 mM	0.0106 mL	0.0528 mL	0.1056 mL	0.2640 mL

Keywords

Ledipasvir (acetone)

31 Cited Publications

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Ledipasvir (acetone)

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Publications Citing Use of MedChemExpress (MCE) Ledipasvir (acetone)

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ledipasvir (acetone)

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Rare Diseases Drug Library

Pediatric Drug 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

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Ledipasvir (acetone)

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ledipasvir (acetone) Related Classifications

HY-15602A Related Classifications