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Ledipasvir

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Catalog No. T6200Cas No. 1256388-51-8
Alias 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.

Ledipasvir

Ledipasvir

😃Good
Purity: 99.96%
Catalog No. T6200Alias GS-5885Cas No. 1256388-51-8
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32In StockIn Stock
2 mg$45In StockIn Stock
5 mg$72In StockIn Stock
10 mg$90In StockIn Stock
25 mg$162In StockIn Stock
50 mg$270In StockIn Stock
100 mg$468In StockIn Stock
500 mg$1,0707-10 days7-10 days
1 mL x 10 mM (in DMSO)$90In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.96%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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 distinguishes itself not only for its substantial replicon potency but also for its low clearance, high bioavailability, and extended half-lives across several species (rat, dog, and monkey) alongside a low predicted clearance in humans. Its pharmacokinetics have been assessed in rats and dogs, demonstrating favorable plasma half-lives (rat 1.83 ± 0.22 hr, dog 2.63 ± 0.18 hr), minimal systemic clearance (CL), and moderate distribution volumes (Vss) exceeding total body water volume[1].
SynonymsGS-5885
Chemical Properties
Molecular Weight889
FormulaC49H54F2N8O6
Cas No.1256388-51-8
SmilesCOC(=O)N[C@@H](C(C)C)C(=O)N1CC2(CC2)C[C@H]1c1ncc([nH]1)-c1ccc2-c3ccc(cc3C(F)(F)c2c1)-c1ccc2nc([nH]c2c1)[C@@H]1[C@H]2CC[C@H](C2)N1C(=O)[C@@H](NC(=O)OC)C(C)C
Relative Density.1.42 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 255 mg/mL (286.84 mM), Sonication is recommended.
Ethanol: 93 mg/mL (104.61 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (5.62 mM), Sonication is recommended.
2% DMSO+40% PEG300+5% Tween 80+53% Saline: 1 mg/mL (1.12 mM), Solution.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.1249 mL5.6243 mL11.2486 mL56.2430 mL
5 mM0.2250 mL1.1249 mL2.2497 mL11.2486 mL
10 mM0.1125 mL0.5624 mL1.1249 mL5.6243 mL
20 mM0.0562 mL0.2812 mL0.5624 mL2.8121 mL
50 mM0.0225 mL0.1125 mL0.2250 mL1.1249 mL
100 mM0.0112 mL0.0562 mL0.1125 mL0.5624 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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