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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
2 mg | $45 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $90 | In Stock | |
25 mg | $162 | In Stock | |
50 mg | $270 | In Stock | |
100 mg | $468 | In Stock | |
500 mg | $1,070 | In Stock | |
1 mL x 10 mM (in DMSO) | $90 | In Stock |
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]. |
Alias | GS-5885 |
Molecular Weight | 889 |
Formula | C49H54F2N8O6 |
Cas No. | 1256388-51-8 |
Smiles | COC(=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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (104.6 mM) Ethanol: 93 mg/mL (104.6 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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