產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg
CAS	1256388-51-8
別名	GS-5885;GS 5885;GS5885
化學(xué)名	GS-5885;GS 5885;GS5885
分子式	C49H54F2N8O6
分子量	889
溶解度	≥ 44.45 mg/mL in DMSO, ≥ 46.9 mg/mL in EtOH with gentle warming
儲(chǔ)存條件	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.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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