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。AT-527 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC90=0.47 μM)。AT-527 具有全基因型抗病毒活性。
货号:ajcx33490
CAS:2241337-84-6
分子式:C24H33FN7O7P.1/2H2O4S
分子量：630.58
溶解度:DMSO : 180 mg/mL (285.45 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AT-527, a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. AT-527 is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). AT-527 has pangenotypic antiviral activity[1][2][3].

AT-511 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[1].In normal human airway epithelial cells, the concentration of AT-511 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[2].

When given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg or 300 mg/kg), AT-527 preferentially delivers high levels of AT-9010 in the liver in vivo[1].

[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.
[3]. Elina Berliba, et al. Safety, pharmacokinetics and antiviral activity of AT-527, a novel purine nucleotide prodrug, in HCV-infected subjects with and without cirrhosis. Antimicrob Agents Chemother. 2019 Sep 30;63(12):e01201-19.