Peramivir Trihydrate 是一种高效、选择性和口服有效的流感病毒神经氨酸酶(NA)抑制剂,对 9 个亚型 NA 抑制作用的IC50值为 0.9-4.3 nM。它是一种环戊烷衍生物,具有抗甲型和乙型流感病毒的活性。
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Peramivir is a neuraminidase inhibitor (IC50: 0.09 nM) which prevents normal processing of virus particles such that virus particles are not released from infected cells. Peramivir is a cyclopentane derivative with activity against influenza A and B viruses.
体外活性
Peramivir(0.025-0.1 mg/kg/day)和法匹拉韦(20-40 mg/kg/day)联用时增加10-50%细胞存活率.Peramivir(0.5 mg/kg/day)对30%的H1N1病毒小鼠有保护效果.Peramivir(1 mg/kg/day)和金刚烷乙胺(5-10 mg/kg/day)联用使体重分别损失1.69和0.69,但在亚致死流感A(H3N2)病毒的小鼠模型中,每天3 mg/kg Peramivir(3 mg/kg/day)和Rimantadine(10-30 mg/kg/day)联用则不影响体重.Peramivir(30 mg/kg)能有效促进感染全身复制H5N1病毒小鼠的生存期.
Cas No.
1041434-82-5
分子式
C15H28N4O4·3H2O
分子量
382.45
别名
BCX 1812 trihydrate;帕拉米韦三水合物;RWJ 270201 trihydrate;BCX-1812;S-021812;RWJ-270201
储存和溶解度
H2O:6.6 mg/mL (17.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years