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Ledipasvir

SKU: orb1688038

Description

Ledipasvir (GS-5885) is a small molecule NS5A inhibitor used in hepatitis C virus (HCV) research. It also acts as an inhibitor of the P-glycoprotein and Breast Cancer Resistance Protein (BCRP) transporters, making it a useful tool for in vitro and in vivo studies of drug efflux and pharmacokinetics.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number1256388-51-8
MW889
Purity99.96%
FormulaC49H54F2N8O6
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
TargetHCV Protease,SARS-CoV
SolubilityEthanol:93 mg/mL (104.61 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (5.62 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:255 mg/mL (286.84 mM);2% DMSO+40% PEG300+5% Tween 80+53% Saline:1 mg/mL (1.12 mM)

Bioactivity

Target IC50
NS5A (1a replicon):34 pM(EC50)|NS5A (1b replicon):4 pM(EC50)
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.
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. Ledipasvir exhibits an EC50 value of 141 nM against the JFH/3a-NS5A replicon.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SARSCoV, SARS coronavirus, SARS-CoV, Inhibitor, inhibit, Hepatitis C virus, HCV Protease, HCV, HCVProtease, Ledipasvir, GS 5885, GS5885, GS-5885, GT1a, GT1b

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

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Protocol Information

Ledipasvir (orb1688038)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 80.00
2 mg
$ 90.00
5 mg
$ 120.00
1 ml x 10 mM (in DMSO)
$ 130.00
10 mg
$ 130.00
25 mg
$ 210.00
50 mg
$ 310.00
100 mg
$ 510.00
500 mg
$ 1,110.00
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