Ledipasvir hydrochloride
Based on 31 publication(s) in Google Scholar
Ledipasvir (GS-5885) hydrochloride 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 hydrochloride is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM.
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- CAS 番号: 2128695-48-5
- 分子式: C49H55ClF2N8O6
- 分子量:925.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Ledipasvir hydrochloride
More- Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
- Lancet Microbe. 2024 Jul;5(7):697-706. [Abstract]
- J Transl Med. 2025 Jan 22;23(1):103. [Abstract]
- Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1922-1927. [Abstract]
- Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876. [Abstract]
- Ann Hepatol. 2019 Nov-Dec;18(6):816-824. [Abstract]
- Pharmaceuticals (Basel). 2022 Feb 18;15(2):242. [Abstract]
- J Gastroenterol. 2019 May;54(5):449-458. [Abstract]
- Antiviral Res. 2017 Mar:139:18-24. [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]
- Viruses. 2023 Apr 17;15(4):981. [Abstract]
- Viruses. 2019 Nov 8;11(11):1039. [Abstract]
- Viruses. 2018 Aug 28;10(9):462. [Abstract]
- Drug Metab Dispos. 2019 Jul;47(7):768-778. [Abstract]
- PLoS One. 2021 May 20;16(5):e0251934. [Abstract]
- PLoS One. 2016 Jul 21;11(7):e0159511. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15:1110-1111:15-24. [Abstract]
- Transpl Infect Dis. 2018 Feb;20(1). [Abstract]
- Neurosci Lett. 2015 Nov 16:609:48-52. [Abstract]
- Biomed Chromatogr. 2022 Sep;36(9):e5427. [Abstract]
- Biomed Pharmacother. 2024 Oct:179:117325. [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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Cell Imaging/Staining
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生物活性
製品説明
IC50 & Target
EC50: 34 pM (GT1a), 4 pM (GT1b)[1]
IC50: 1.62 Μm (SARS-CoV 3CLpro)[3]
体外実験
Ledipasvir hydrochloride 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 hydrochloride is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay[1]. Ledipasvir hydrochloride 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. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2128695-48-5
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分子量 925.46
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分子式 C49H55ClF2N8O6
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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.Cl
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別名
GS-5885 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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 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 hydrochloride 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 -
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
Ledipasvir hydrochloride purchased from MedChemExpress. Usage Cited in: Viruses. 2023 Apr 17;15(4):981. [Abstract]
epresentative images of LDs in cells treated with 100 × EC50 Ledipasvir (LDV) or CsA for 8 h. The scale bar represents 100 µm.
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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 -
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プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Ledipasvir hydrochloride 関連分類
HY-15602C 関連分類
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