1. Anti-infection
  2. HCV
    SARS-CoV
  3. Ledipasvir hydrochloride

Ledipasvir hydrochloride (Synonyms: GS-5885 hydrochloride)

Cat. No.: HY-15602C
Handling Instructions

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.

For research use only. We do not sell to patients.

Ledipasvir hydrochloride Chemical Structure

Ledipasvir hydrochloride Chemical Structure

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Top Publications Citing Use of Products

    Ledipasvir hydrochloride purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Jun;59(6):3482-92.

    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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    Description

    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[3].

    IC50 & Target

    EC50: 34 pM (GT1a), 4 pM (GT1b)[1]
    IC50: 1.62 Μm (SARS-CoV 3CLpro)[3]

    In Vitro

    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].

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

    In Vivo

    Ledipasvir hydrochloride 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 hydrochloride is measured in rats and dogs. Ledipasvir shows good half-lives (rat 1.83 hr, dog 2.63 hr) in plasma, low systemic clearance (CL), and moderate volumes of distribution (Vss) that are greater than total body water volume[1].

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

    Molecular Weight

    925.46

    Formula

    C49H55ClF2N8O6

    SMILES

    O=C(OC)N[[email protected]](C(N([[email protected]](C1=NC=C(C2=CC(C(F)(F)C3=C4C=CC(C5=CC=C6N=C([[email protected]]7N(C([[email protected]@H](NC(OC)=O)C(C)C)=O)[[email protected]]8([H])CC[[email protected]@]7([H])C8)NC6=C5)=C3)=C4C=C2)N1)C9)CC%109CC%10)=O)C(C)C.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
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