Bemnifosbuvir hemisulfate (Synonyms: AT-527)
目录号: PL11156 纯度: ≥99%
CAS No. :2241337-84-6
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中文名称
Bemnifosbuvir hemisulfate
中文别名
AT-527 半个硫酸盐;化合物BEMNIFOSBUVIR HEMISULFATE
英文名称
Bemnifosbuvir hemisulfate
英文别名
AT527;GTPL11295;propan-2-yl (2S)-2-[[[(3R,4R,5R)-5-[2-amino-6-(methylamino)purin-9-yl]-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate;AT-527;AT-527(Bemnifosbuvir);Bemnifosbuvir hemisulfate;Bemnifosbuvir hemisulfate (RG-6422;Inhibitor,antiviral,phosphoramidate,HCV,nucleotide,SARS-CoV,pangenotypic,Bemnifosbuvir hemisulfate,AT 527,AT527,guanosine,SARS coronavirus,Hepatitis C virus,inhibit
Cas No.
2241337-84-6
分子式
C24H33FN7O7P
分子量
581.53
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Bemnifosbuvir hemisulfate (AT-527),AT-511 的半硫酸盐,是鸟苷核苷酸前药,是一种有效的具有口服活性的 HCV 病毒复制抑制剂。Bemnifosbuvir hemisulfate 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC90=0.47 μM)。Bemnifosbuvir hemisulfate 具有全基因型抗病毒活性。
生物活性
Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC 90 =0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity.
性状
Solid
IC50 & Target[1][2]
EC50: 5-28 nM (HCV)
EC90: 0.47 μM (SARS-CoV-2)
体外研究(In Vitro)
Bemnifosbuvir hemisulfate has pan-genotypic antiviral activities that inhibits HCV genotype 1a (HCV GT1a), HCV GT1b, HCV GT2a, HCV GT3a, HCV GT4a, and HCV GT5a replication with EC50 values of 12.8 nM, 12.5 nM, 9.2 nM, 10.3 nM, 14.7 nM, and 28.5 nM, respectively.
In normal human airway epithelial cells, the concentration of Bemnifosbuvir hemisulfate required to inhibit replication of SARS-CoV-2 by EC90 is 0.47 μM, very similar to its EC90 against HCoV-229E, HCoV-OC43 and SARS-CoV in Huh-7 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
When given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg or 300 mg/kg), Bemnifosbuvir hemisulfate preferentially delivers high levels of AT-9010 in the liver in vivo. 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Steven S Good, et al. Preclinical evaluation of AT-527, a novel guanosine nucleotide prodrug with potent, pan-genotypic activity against hepatitis C virus. PLoS One. 2020 Jan 8;15(1):e0227104.
[2]. Steven S Good, et al. AT-527, a double prodrug of a guanosine nucleotide analog, is a potent inhibitor of SARS-CoV-2 in vitro and a promising oral antiviral for treatment of COVID-19. Antimicrob Agents Chemother. 2021 Feb 8;AAC.02479-20.
溶解度数据
In Vitro: DMSO : 180 mg/mL (285.45 mM; Need ultrasonic)H2O : ≥ 100 mg/mL (158.58 mM)
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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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