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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Proteases>HCV Protease Inhibitors> Ledipasvir
	Ledipasvir
  • 	Ledipasvir
  • 	Ledipasvir

Ledipasvir NEW

Price $6 $5 $1
Package 1KG 25KG 100KG
Min. Order: 1KG
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-29

Product Details

Product Name: Ledipasvir CAS No.: 1256388-51-8
Min. Order: 1KG Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/29
Lead time: In stock Packaging: bottle/drum/bucket/IBC, as request.
Delivery: By sea, by air, by express Origin: Manufacturer
Name: Sun

1. Product information

Names

Nameledipasvir
SynonymMore Synonyms

 Ledipasvir Biological Activity

DescriptionLedipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
Related Catalog
Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease
Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection
Target

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

In VitroLedipasvir 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 VivoLedipasvir 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].
Animal AdminRats, Dogs and Monkeys[1] Pharmacokinetic studies are performed in male naı̈ve Sprague-Dawley(SD) rats, non-naive 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.
References

[1]. Link JO, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46

[2]. Hernandez D, et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013 May;57(1):13-8.

 Chemical & Physical Properties

Density1.4±0.1 g/cm3
Molecular FormulaC49H54F2N8O6
Molecular Weight889.000
Exact Mass888.413452
PSA174.64000
LogP6.77
Index of Refraction1.677

 Safety Information

Hazard CodesXi
Safety Phrases24/25
RIDADR3077
HS Code29333990

 Synonyms

Carbamic acid, N-[(1S)-1-[[(6S)-6-[5-[9,9-difluoro-7-[2-[(1R,3S,4S)-2-[(2S)-2-[(methoxycarbonyl)amino]-3-methyl-1-oxobutyl]-2-azabicyclo[2.2.1]hept-3-yl]-1H-benzimidazol-6-yl]-9H-fluoren-2-yl]-1H-imidazol-2-yl]-5-azaspiro[2.4]hept-5-yl]carbonyl]-2-methylpropyl]-, methyl ester
Methyl [(2S)-1-{(1R,3S,4S)-3-[5-(9,9-difluoro-7-{2-[(6S)-5-{(2S)-2-[(methoxycarbonyl)amino]-3-methylbutanoyl}-5-azaspiro[2.4]hept-6-yl]-1H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzimidazol-2-yl]-2-azabicyclo[2.2.1]hept-2-yl}-3-methyl-1-oxo-2-butanyl]carbamate
UNII-013TE6E4WV
Ledipasvir
GS-5885



2. Packaging

For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                     Or smaller package 1kg/bottle, 10kgs/bottle as request. 


Article illustrationArticle illustration


3. Shipping

Article illustration


4. Contact information

For more details, pls contact us freely.

Email address : Sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137





Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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