Product Description

Product Name: Ledipasvir

CAS No.: 1256388-51-8

Information: HCV NS5A protein inhibitor

Other Names: GS 5885; GS5885; GS-5885;Ledipasvir;GS-5885/Ledipasvir;gs-5885/gs5885;Ledipasvir / GS 5885;GS 588

Chemical Name: GS-5885; GS 5885; GS5885

Canonical SMILES: CC([C@@](/N=C(OC)\O)([H])C(N1CC2(C[C@@]1([H])C3=NC=C(N3)C4=CC5=C(C6=C(C5(F)F)C=C(C7=CC(N8)=C(N=C8[C@]9([H])[C@@]%10([H])CC[C@](N9C([C@](/N=C(OC)\O)([H])C(C)C)=O)([H])C%10)C=C7)C=C6)C=C4)CC2)=O)C

MF: C49H54F2N8O6

MW: 888.999860000001

Purity: 99%

Type: Anti HCV Agents

Grade Standard: Medicine Grade

Model Number: API-ledipasvir

Solubility: Soluble in DMSO > 10 mM 

Storage: Store at -20°C 

General tips: For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. 

Shipping Condition: Evaluation sample solution: ship with blue ice. All other available size: ship with RT , or blue ice upon request

Background:Ledipasvir is an inhibitor of the hepatitis C virus replication with IC50 value of 141 nM [1].

Hepatitis C virus (HCV) is an enveloped (+)-single stranded RNA virus, which is the cause of hepatitis C and some cancer lymphomas. The viral RNA is replicated in host cell via RNA-dependent RNA polymerase of HIV and then assembled into virions. The zinc-binding phosphoprotein NS5A protein is translated from HCV genome, which plays important role in the virus replication process. It may act as an transcriptional activator for NS5A RNA replication system and also the mediator of virion assembly.

Ledipasvir is a specific inhibitor of HCV NS5A protein to inhibit HCV replication in the HCV subgenomic replicon system. NS5A replication complex inhibitors are novel antiviral factors for HCV treatment. Typically, these inhibitors have high efficiency and low viral resistance when compared to traditional HCV replication inhibitor targeted on NS3 helicase and NS5B RNA polymerasae. NS5A inhibitors are supposed to bind across the NS5A dimer interface, proximal to N-terminal domain 1. The binding is thought to distort dimer association directly or allosterically, which may disrupt NS5A function in HCV RNA replication [2]. When a JFH1/3a-NS5A hybrid replicon was used to assess susceptibility to NS5A, another inhibitor DCV was shown to be more potent than ledipasvir. Additionally, NS5A-A30K and -Y93H variants exhibited reduced sensitivity to ledpasvir (EC50 value of 1770 nM and 4300 nM respectively) [1].

In clinical trials, it was observed ledpasvir was well tolerated and exhibited median maximal reduction of HCV RNA ranging from 2.3 log10 IU/ml to 3.3 log10 IU/ml. Emax modeling also showed administration of 30 mg ledpasvir after 3 days resulted in >95% maximal response of HCV RNA reduction to genotype 1a.Finally, it was also observed that HCV RNA was more sustained in genotype 1b compared to 1a [3].

Brand Name:Huavet

Place of Origin: Shaanxi,China (Mainland)

Usage: Pharmaceutical Intermediates

Sample: Available

COA: Available

MSDS: Available

Spectrum: Available

Inventory status: in stock

Packaging Details: 1g,5g,10g,50g,100g/bottle, 1kg/tin for trial order 25kg/drum for commercial quantity or specific packing required by customer of Ledipasvir

Delivery Detail: Prompt shipment

 

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