特考韦瑞 T17026

Product Introduction
Bioactivity


英文名: Tecovirimat

描述: 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。

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (132.86 mM)


关键字: Tecovirimat | ST 246 | ST246

相关产品: ONO-5334 | MIV-247 | KGP94 | Odanacatib | Aureusimine B | Cysteine protease inhibitor-2 | PMSF | Papain | LV-320 | Cathepsin X-IN-1

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Protease Inhibitor Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途