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)