1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    HCV Protease

Ledipasvir (Synonyms: GS-5885)

Cat. No.: HY-15602 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.
Ledipasvir Chemical Structure

Ledipasvir Chemical Structure

CAS No. : 1256388-51-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 84 In-stock
10 mg USD 108 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Ledipasvir:

    Ledipasvir 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.

    Ledipasvir purchased from MCE. Usage Cited in: Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.

    Simeprevir inhibits DNA damage repair following irradiation. U251, BT474, and HepG2 cells are pretreated with Simeprevir or DMSO and irradiated at a dose of 6 Gy. After 6 hours, prolongation of γH2AX foci is detected in Simeprevir-treated cells along with decreased phosphorylation of DNA-PKcs, indicating impaired nonhomologous end-joining repair.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    EC50: 34 pM (GT1a), 4 pM (GT1b)[1]

    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 and low predicted clearance in human. The pharmacokinetics of Ledipasvir is measured in rats and dogs. 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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.1249 mL 5.6243 mL 11.2486 mL
    5 mM 0.2250 mL 1.1249 mL 2.2497 mL
    10 mM 0.1125 mL 0.5624 mL 1.1249 mL
    Please refer to the solubility information to select the appropriate solvent.
    Animal Administration
    [1]

    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) [1].
    Oral dosing is administered by gavage in a vehicle containing 5% ethanol, 45% PEG 400, and 50% of 50 mM citrate buffer, pH 3 [1].

    Rats, Dogs and Monkeys[1]
    Pharmacokinetic studies are performed in male naı̈ve Sprague-Dawley(SD) rats, non-naı̈ve 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    889.0

    Formula

    C₄₉H₅₄F₂N₈O₆

    CAS No.

    1256388-51-8

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Ledipasvir
    Cat. No.:
    HY-15602
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