Ledipasvir
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 3CLpro inhibitor with an IC50 of 1.62 μM.
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- Pureté: 99.69%
- CAS No.: 1256388-51-8
- Formule: C49H54F2N8O6
- Masse moléculaire:889.00
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Ledipasvir
More- Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
- Lancet Microbe. 2024 Jun 15:S2666-5247(24)00041-7. [Abstract]
- Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1922-1927. [Abstract]
- J Transl Med. 2025 Jan 22;23(1):103. [Abstract]
- Biomed Pharmacother. 2024 Sep 2:179:117325. [Abstract]
- Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876. [Abstract]
- J Gastroenterol. 2019 May;54(5):449-458. [Abstract]
- Pharmaceuticals (Basel). 2022 Feb 18;15(2):242. [Abstract]
- Antimicrob Agents Chemother. 2015;59(6):3482-92. [Abstract]
- Antimicrob Agents Chemother. 2015 May;59(5):2496-507. [Abstract]
- Antimicrob Agents Chemother. 2014 Sep;58(9):5386-94. [Abstract]
- Ann Hepatol. Nov-Dec 2019;18(6):816-824. [Abstract]
- Drug Metab Dispos. 2019 Jul;47(7):768-778. [Abstract]
- Antiviral Res. 2017 Mar;139:18-24. [Abstract]
- Viruses. 2023 Apr 17;15(4):981. [Abstract]
- Viruses. 2019 Nov 8;11(11):1039. [Abstract]
- Viruses. 2018 Aug 28;10(9). pii: E462. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15:1110-1111:15-24. [Abstract]
- PLoS One. 2021 May 20;16(5):e0251934. [Abstract]
- Transpl Infect Dis. 2018 Feb;20(1). [Abstract]
- PLoS One. 2016 Jul 21;11(7):e0159511. [Abstract]
- Neurosci Lett. 2015 Nov 16;609:48-52. [Abstract]
- Biomed Chromatogr. 2022 Sep;36(9):e5427. [Abstract]
- 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.
Customer Validation & Images
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Activité biologique
EC50: 34 pM (GT1a), 4 pM (GT1b)[1]
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | EC50 |
210 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
| Huh-7 | EC50 |
210 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
| Huh-7 | EC50 |
27 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
| Huh-7 | EC50 |
27 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
| Huh-7 | EC50 |
31 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
| Huh-7 | EC50 |
4 pM
Compound: 39, GS-5885, ledipasvir
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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
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[PMID: 24320933] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1256388-51-8
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Appearance Solid
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Masse moléculaire 889.00
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Formule C49H54F2N8O6
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Color Light yellow to yellow
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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
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Synonyms
GS-5885
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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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
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.
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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 -
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Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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.
Pureté et documentation
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Fiche technique (281 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
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