Tecovirimat 是一种核心蛋白半胱氨酸蛋白酶抑制剂，可能用于治疗天花感染。Tecovirimat 是一种新型抗病毒药物，对多种正痘病毒具有有效和选择性的活性（EC50：约 10 nM）。通过靶向病毒 p37 蛋白直系同源物来抑制正痘病毒的排出。迄今为止，Tecovirimat 已在所有小动物和非人类灵长类动物预防和治疗痘病毒引起的疾病模型中显示出功效。

Tecovirimat is a core protein cysteine protease inhibitor potentially for treatment of smallpox infection.Tecovirimat is a novel antiviral potent and selective activity against multiple orthopoxviruses (EC50: about 10 nM). that inhibits the egress of orthopoxviruses by targeting viral p37 protein orthologs.Tecovirimat has shown efficacy in all small animal and nonhuman primate prophylaxis and therapeutic efficacy models of poxvirus-induced disease tested to date.

ST-246 was evaluated for activity against cowpox virus (CV), vaccinia virus (VV), and ectromelia virus (ECTV) and had an in vitro 50% effective concentration (EC50) of 0.48 microM against CV, 0.05 microM against VV, and 0.07 microM against ECTV.?The selectivity indices were >208 and >2,000 for CV and VV, respectively.?The in vitro antiviral activity of ST-246 was significantly greater than that of cidofovir, which had an EC50 of 41.1 microM against CV and 29.2 microM against VV, with selectivity indices of >7 and >10, respectively[2].

ST-246 administered once daily by oral gavage to mice infected intranasally with CV beginning 4 h or delayed until 72 h postinoculation was highly effective when given for a 14-day duration using 100, 30, or 10 mg/kg of body weight.?When 100 mg/kg of ST-246 was administered to VV-infected mice, a duration of 5 days was sufficient to significantly reduce mortality even when treatment was delayed 24 h postinoculation.?Viral replication in liver, spleen, and kidney, but not lung, of CV- or VV-infected mice was reduced by ST-246 compared to levels for vehicle-treated mice.?When 100 mg/kg of ST-246 was given once daily to mice infected by the intranasal route with ECTV, treatment for 10 days prevented mortality even when treatment was delayed up to 72 h after viral inoculation.?Viral replication in target organs of ECTV-infected mice was also reduced[2].

869572-92-9

C19H15F3N2O3

376.33

ST-246;特考韦瑞

DMSO:50 mg/mL (132.86 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years