Presatovir是一種新型的呼吸道合胞病毒(RSV)融合 F 蛋白抑制劑,具有針對廣泛菌株的強效抗病毒活性,通過結(jié)合病毒表面的 F 蛋白起作用。Presatovir is an antiviral drug which was developed as a treatment for respiratory syncytial virus(RSV). A mean EC50 = 0.43 nM was found toward a panel of 75 RSV A and B clinical isolates and dose-dependent antiviral efficacy in the cotton rat model of RSV infection. Oral bioavailability in preclinical species ranged from 46 to 100%, with evidence of efficient penetration into lung tissue[3]. Presatovir exhibited potent antiviral activity with a mean EC50 value of 0.35 ± 0.14 nM against a broad range of RSV isolates and a low cytotoxicity in vitro. Presatovir exhibited low cytotoxicity in uninfected HEp-2 cells with a CC50 value of 48,900 ± 5,600 nM. Presatovir blocked entry of RSV into host cells, but did not inhibit binding of RSV to the cell surface in temperature shift experiments. Presatovir inhibited RSV replication with an EC50 value of 0.10 ± 0.05 nM [4].
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