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Ledipasvir D-tartrate

Catalog No. T11832   CAS 1502654-87-6
Synonyms: GS-5885 D-tartrate

Ledipasvir D-tartrate with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon. is an inhibitor of the hepatitis C virus NS5A.

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Ledipasvir D-tartrate Chemical Structure
Ledipasvir D-tartrate, CAS 1502654-87-6
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ledipasvir D-tartrate with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon. is an inhibitor of the hepatitis C virus NS5A.
Targets&IC50 GT1b: 4 pM , GT1a:(EC50)34 pM
In vitro 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].?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.
In vivo 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].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.
Synonyms GS-5885 D-tartrate
Molecular Weight 1039.104
Formula C53H60F2N8O12
CAS No. 1502654-87-6

Storage

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

Solubility Information

DMSO: 28 mg/mL (26.95 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.

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Keywords

Ledipasvir D-tartrate 1502654-87-6 Others GS-5885 D-tartrate Ledipasvir D tartrate Ledipasvir Dtartrate inhibitor inhibit

 

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