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Ledipasvir acetone HCV inhibitor

Cat.No.S4434

Ledipasvir (GS-5885) acetone is the active ingredient of Ledipasvir. Ledipasvir is a potent, oral active inhibitor of the hepatitis C virus (HCV) NS5A with EC50 of 31 pM and 4 pM against GT1a and GT1b replicon, respectively.
Ledipasvir acetone HCV inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 947.08

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Quality Control

Batch: S443401 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (105.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 947.08 Formula

C52H60F2N8O7

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1441674-54-9 -- Storage of Stock Solutions

Synonyms GS-5885 acetone Smiles COC(=O)NC(C(C)C)C(=O)N1CC2(CC2)CC1C3=NC=C([NH]3)C4=CC5=C(C=C4)C6=C(C=C(C=C6)C7=CC8=C(C=C7)N=C([NH]8)C9C%10CCC(C%10)N9C(=O)C(NC(=O)OC)C(C)C)C5(F)F.CC(C)=O

Mechanism of Action

Targets/IC50/Ki
GT1b replicon
(Cell-free assay)
4 pM(EC50)
GT1a replicon
(Cell-free assay)
31 pM(EC50)
In vitro

Ledipasvir acetone induces HCV clearance, inhibits STAT3 protein levels and restores HNF4A expression.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03903185 Completed
Hepatitis C Chronic|Hematologic Malignancy
Ain Shams University|Cairo University
 March 1 2019 Phase 1|Phase 2
NCT03639207 Withdrawn
Hepatitis C Virus
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 June 15 2018 --
NCT05091008 Completed
Hepatitis C Chronic
Mansoura University Children Hospital
 March 1 2018 Phase 2

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