| 中文名称 |
Elbasvir
|
| 中文别名 |
依巴司韦
|
| 英文名称 |
Elbasvir
|
| 英文别名 |
MK 8742;Elbasvir;MK-8742;Methyl N-[(2S)-1-[(2S)-2-[5-[(6S)-10-[2-[1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidi
|
| Cas No. |
1370468-36-2
|
| 分子式 |
C49H55N9O7
|
| 分子量 |
882.02
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
Elbasvir (MK-8742) 是丙型肝炎病毒非结构蛋白5A (HCV NS5A) 抑制剂, 对基因型1a,1b和2a的 EC50 分别为4,3 和3 nM。
|
| 产品详情 |
Elbasvir (MK-8742) 是丙型肝炎病毒非结构蛋白5A (HCV NS5A) 抑制剂, 对基因型1a,1b和2a的 EC50 分别为4,3 和3 nM。
|
| 生物活性 |
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC 50 s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
EC50: 4 nM (HCV 1a), 3 nM (HCV 1b), 3 nM (HCV 2a)
|
| 体外研究(In Vitro) |
Elbasvir shows potent activity against genotype 1a and 1b replicons, with EC90 of 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. Elbasvir inhibits genotype 3 replicons with EC90 of 0.12 nM. Elbasvir (0.06 nM, 0.6 nM, and 6 nM) demonstrates dose-dependent suppression of resistant genotype 1a replicons, illustrated by the reductions in colony counts at higher doses. Elbasvir is highly potent against HCV replicons bearing NS5A sequences from GT1a, -1b, -2a(31L), -3a, -4a, -5a, and -6, with EC50s in the low-picomolar range. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| ClinicalTrial |
|
| 参考文献 |
[1]. Liu R, 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):6922-6929.[2]. Lahser FC, 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 A
|
| 溶解度数据 |
In Vitro: DMSO : ≥ 50 mg/mL (56.69 mM)配制储备液
|
[1]. Liu R, 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):6922-6929.[2]. Lahser FC, 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 A
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。