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Ledipasvir

Catalog No. T6200   CAS 1256388-51-8
Synonyms: GS-5885

Ledipasvir (GS-5885) is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ledipasvir Chemical Structure
Ledipasvir, CAS 1256388-51-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 90.00
25 mg In stock $ 162.00
50 mg In stock $ 270.00
100 mg In stock $ 468.00
500 mg In stock $ 1,070.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.46%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ledipasvir (GS-5885) is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor.
Targets&IC50 NS5A(1b replicon):4 pM(EC50), NS5A(1a replicon):34 pM(EC50)
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].
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 as well as low predicted clearance in human. The pharmacokinetics of Ledipasvir is measured in rats and dogs. Ledipasvir exhibits 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].
Synonyms GS-5885
Molecular Weight 889
Formula C49H54F2N8O6
CAS No. 1256388-51-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (104.6 mM)

Ethanol: 93 mg/mL (104.6 mM)

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Approved Drug Library Clinical Compound Library Anti-Cancer Compound Library Bioactive Compound Library Drug Repurposing Compound Library

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Keywords

Ledipasvir 1256388-51-8 Microbiology/Virology Proteases/Proteasome HCV Protease SARS-CoV inhibit HCV Inhibitor SARS coronavirus GS-5885 GS 5885 GS5885 Hepatitis C virus inhibitor

 

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