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编 号:F754819
分子式:C27H29N3O2
分子量:427.54
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生物活性:
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 μg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice.

体内研究:
SIMR3030 (25、50、100 mg/kg;I.p.;每日一次,持续 14 天) 在实验小鼠模型中表现出较好的安全性。Animal Model:18-25 g, adult female Balb/c mice
Dosage:25, 50, 100 mg/kg
Administration:I.p.; daily for 14 days
Result:Showed no signs of toxicity or weight loss were noticed during 12.5 and 25 mg/kg multiple-dose studies for 14 days, no signs of toxicity or weight loss were noticed during 12.5 and 25 mg/kg multiple-dose studies for 14 days.

体外研究:
SIMR3030 (0-100 μg/mL) 显示抗病毒活性,对 SARS-CoV-2 和 MERS-CoV 的 IC50 值分别为 12.1、6.206 μg/mL。SIMR3030 (20 μg/mL; 1, 6, 12 h) 降低 Caco-2 细胞中的 SARS-CoV spike、ORF1b、IFN-α、IL-6 mRNA 表达水平。
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