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Elbasvir {[allProObj[0].p_purity_real_show]}

货号:A155998 同义名: MK-8742

Elbasvir是一种丙型肝炎病毒(HCV)非结构蛋白 5A(NS5A)抑制剂,可用于治疗慢性 HCV 感染。

Elbasvir 化学结构 CAS号:1370468-36-2
Elbasvir 化学结构
CAS号:1370468-36-2
Elbasvir 3D分子结构
CAS号:1370468-36-2
Elbasvir 化学结构 CAS号:1370468-36-2
Elbasvir 3D分子结构 CAS号:1370468-36-2
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Elbasvir 纯度/质量文件 产品仅供科研

货号:A155998 标准纯度: {[allProObj[0].p_purity_real_show]}
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Elbasvir 生物活性

描述 Non-structural protein 5A (NS5A) is important for RNA synthesis and virus assembly making it as an attractive target for intervention in chronic Hepatitis C virus (HCV) infection[3]. Elbasvir is a small molecule inhibitor of NS5A of HCV being developed as a component of treatment regimens for chronic HCV infection. In the 3-day replicon assay, the EC90 of elbasvir was 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. The EC90 of elbasvir ranged from 0.01 to 0.02 nM for genotype 1a and 0.01 to 0.03 nM for genotype 1b. In a phase 1 study, elbasvir once daily for 5 days resulted in mean reductions in HCV RNA levels of 3.7-5.1 log10 IU/mL in patients with genotype 1a or 1b infections when given 5-50 mg/day and of ~3 log10 IU/mL in patients with genotype 3 when given 50 or 100 mg/day. In later phase 2 trials, treatment with elbasvir combined with grazoprevir (an investigational once-daily NS3/4A-protease inhibitor) ± ribavirin for 12 weeks produced SVR12 (sustained virologic response) rates of 87-98% for patients with genotype-1 infections[4].

Elbasvir 参考文献

[1]Lahser FC, Bystol K, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64.

[2]Liu R, Curry S, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-9.

[3]Lahser FC, Bystol K, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64

[4]Liu R, Curry S, McMonagle P, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-9

Elbasvir 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.13mL

0.23mL

0.11mL

5.67mL

1.13mL

0.57mL

11.34mL

2.27mL

1.13mL

Elbasvir 技术信息

CAS号1370468-36-2
分子式C49H55N9O7
分子量 882.02
SMILES Code O=C([C@@H](NC(OC)=O)C(C)C)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C4C(C=C5N4[C@@H](OC6=CC(C7=CN=C(N7)[C@@H]8CCCN8C([C@@H](NC(OC)=O)C(C)C)=O)=CC=C56)C9=CC=CC=C9)=C3
MDL No. MFCD30829850
别名 MK-8742
运输蓝冰
InChI Key BVAZQCUMNICBAQ-PZHYSIFUSA-N
Pubchem ID 71661251
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(56.69 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
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