Avoralstat

激肽释放酶和TMPRSS2的抑制剂；抑制分离的人血浆中的激肽释放酶活性（EC50s=1.14-11.1nM）；抑制TMPRSS2（IC50=2.73nM）；抑制SARS-CoV-2假病毒进入Calu-32B4细胞（EC50=0.7µM）；以30mg/kg的剂量分别降低或预防SARS-CoV-2感染或预防的Ad5-hACE2小鼠模型中肺病毒滴度的积累。An inhibitor of kallikrein and TMPRSS2; inhibits kallikrein activity in isolated human plasma (EC50s = 1.14-11.1 nM); inhibits TMPRSS2 (IC50 = 2.73 nM); inhibits SARS-CoV-2 pseudovirus entry into Calu-3 2B4 cells (EC50 = 0.7 µM); reduces or prevents the accumulation of lung viral titers in Ad5-hACE2 mouse models of SARS-CoV-2 infection or prophylaxis, respectively, at 30 mg/kg.分子式C28H27N5O5分子量513.6O=C(C1=C(C2=C(C(NC3=CC=C(C(N)=N)C=C3)=O)C=C(C=C)C(OC)=C2)C=CC(C(NCC4CC4)=O)=N1)O