| Description | 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. |
| In vitro | Tecovirimat 对牛痘病毒（CV）、疱疹病毒（VV）和鼠疫病毒（ECTV）的活性进行了评估，其体外对CVD 50%有效浓度（EC50）分别为0.48μM、对VV 的 0.05μM和对ECTV 的0.07μM。其选择性指数对于CV和VV分别>208和>2000。与cidofovir相比，Tecovirimat 的体外抗病毒活性显著增强，cidofovir对CV的EC50为41.1μM和对VV的EC5029.2μM，[2]。 |
| In vivo | Tecovirimat 通过口腔灌胃每日一次给予经鼻孔接种CV的小鼠，在接种后4小时或延迟至72小时开始治疗，使用100、30或10 mg/kg体重进行14天的疗程，显示出高效性。当给予VV感染小鼠100 mg/kg的Tecovirimat 时，即使治疗延迟至接种后24小时，5天的治疗期足以显著降低死亡率。Tecovirimat 与对照组相比，能减少CV或VV感染小鼠的肝脏、脾脏和肾脏中的病毒复制，但肺部除外。使用100 mg/kg的Tecovirimat ，通过鼻腔途径感染ECTV的小鼠，每日一次治疗10天，即使在病毒接种后72小时内开始治疗，也能防止死亡。ECTV感染小鼠的靶器官中病毒复制同样得到降低。 |
| Synonyms | ST-246, 特考韦瑞 |
| molecular weight | 376.33 |
| Molecular formula | C19H15F3N2O3 |
| CAS | 869572-92-9 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (106.29 mM), Sonication is recommended. |
| References | 1. Yang G, et al. An orally bioavailable antipoxvirus compound (ST-246) inhibits extracellular virus formation and protects mice from lethal orthopoxvirus Challenge. J Virol. 2005 Oct;79(20):13139-49. 2. Quenelle DC, et al. Efficacy of delayed treatment with ST-246 given orally against systemic orthopoxvirus infections in mice. Antimicrob Agents Chemother. 2007 Feb;51(2):689-95. |