NVR 3-778
目录号: PL02680 纯度: ≥99%
CAS No. :1445790-55-5
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中文名称
NVR 3-778
中文别名
4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide
英文名称
NVR 3-778
英文别名
4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide;4-Fluoranyl-3-(4-Oxidanylpiperidin-1-Yl)sulfonyl-~{n}-[3,4,5-Tris(Fluoranyl)phenyl]benzamide;NVR 3-778;4-Fluoro-3-[(4-hydroxy-1-piperidinyl)sulfonyl]-N-(3,4,5-trifluorophenyl)benzamide;BDBM50535698;4-fluoro-3-(4-hydroxypiperidin-1-yl)sulfonyl-N-(3,4,5-trifluorophenyl)benzamide
Cas No.
1445790-55-5
分子式
C18H16F4N2O4S
分子量
432.39
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
NVR 3-778 是一种首创、口服有效的 HBV CAM (衣壳组装调制剂),属于 SBA 类,具有抗 HBV 活性。
生物活性
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
性状
Solid
IC50 & Target[1][2]
HBV
体外研究(In Vitro)
NVR 3-778 targets HBV core protein and inhibits viral replication.
NVR 3-778 inhibits the generation of infectious HBV DNA-containing virus particles with a mean antiviral with an EC50 of 0.40?μM in HepG2.2.15 cells.
NVR 3-778 exhibits pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication.
NVR 3-778 inhibits pregenomic RNA encapsidation, viral replication, and the production of HBV DNA- and HBV RNA-containing particles.
NVR 3-778 also inhibits de novo infection and viral replication in primary human hepatocytes with EC50s of 0.81?μM against HBV DNA and between 3.7μM and 4.8?μM against the production of HBV antigens and intracellular HBV RNA.
The EC50 values of NVR 3-778 are increased by 4.5-, 9.3-, and 15.8-fold in the presence of 10%, 20%, and 40% human serum,
体内研究(In Vivo)
NVR 3-778 (1.5?mg/kg; i.g.) displays the mean C max and AUC 0–inf values of 0.56?μg/ml and 3.50?μg·h/ml, respectively, in dogs following oral administration. And the mean oral bioavailability is determined to be 84.6%.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[1]. Lam AM, et al. Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus. Antimicrob Agents Chemother. 2018 Dec 21;63(1).
溶解度数据
In Vitro: DMSO : 250 mg/mL (578.18 mM; Need ultrasonic)配制储备液
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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。

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