产品说明书

Tecovirimat

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Chemical Structure| 869572-92-9 同义名 : ST-246;SIGA-246;TPOXX
CAS号 : 869572-92-9
货号 : A240633
分子式 : C19H15F3N2O3
纯度 : 98%
分子量 : 376.329
MDL号 : MFCD11973644
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(279.01 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Tecovirimat is a potent, selective and orally bioavailable antipoxvirus compound active against multiple orthopoxviruses, including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), and variola viruses, with EC50 value of 0.01μM for Vaccinia virus in CPE assays. It inhibited plaque formation, virus-induced CPE and extracellular virus production at 5μM. Treatment with oral administration of Tecovirimat, at dose of 50 mg/kg twice a day for 14 days, protected BALB/c mice from lethal infection by vaccinia virus strain IHD-J, A/NCr mice from lethal infection by ectromelia virus[4]. Tecovirimat is FDA-approved for the treatment of human smallpox disease caused by Variola virus in adults and children[5].
作用机制 Tecovirimat blocks interaction of p37 with Rab9 and TIP47. Thus, ST-246 prevents wrapping complex formation by inhibiting interaction of p37 with components of LE-transport vesicle biogenesis[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.29mL

2.66mL

1.33mL

26.57mL

5.31mL

2.66mL

参考文献

[1]Duraffour S, Lorenzo MM, et al. ST-246 is a key antiviral to inhibit the viral F13L phospholipase, one of the essential proteins for orthopoxvirus wrapping. J Antimicrob Chemother. 2015 May;70(5):1367-80.

[2]Mucker EM, Goff AJ, et al. Efficacy of tecovirimat (ST-246) in nonhuman primates infected with variola virus (Smallpox). Antimicrob Agents Chemother. 2013 Dec;57(12):6246-53.

[3]Grosenbach DW, Jordan R, Hruby DE. Development of the small-molecule antiviral ST-246 as a smallpox therapeutic. Future Virol. 2011 May;6(5):653-671. doi: 10.2217/fvl.11.27. PMID: 21837250; PMCID: PMC3151656.

[4]Yang G, Pevear DC, Davies MH, Collett MS, Bailey T, Rippen S, Barone L, Burns C, Rhodes G, Tohan S, Huggins JW, Baker RO, Buller RL, Touchette E, Waller K, Schriewer J, Neyts J, DeClercq E, Jones K, Hruby D, Jordan R. 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. doi: 10.1128/JVI.79.20.13139-13149.2005. PMID: 16189015; PMCID: PMC1235851.

[5]Guidance for Tecovirimat Use Under Expanded Access Investigational New Drug Protocol during 2022 U.S. Monkeypox Outbreak