Tecovirimat monohydrate  (Synonyms: ST-246 monohydrate)

Tecovirimat (ST-246) monohydrate is the monohydrate form of Tecovirimat (HY-14805). Tecovirimat monohydrate is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat monohydrate is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat monohydrate targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat monohydrate exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat monohydrate could be used in the study for orthopoxvirus-induced diseases^{[1][2][3][4][5]}.

Tecovirimat monohydrate (0-50 μM, 3 days) is a potent and specific inhibitor of orthopoxvirus replication that is active against a broad spectrum of orthopoxviruses^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tecovirimat monohydrate (50 mg/kg, oral gavage, twice a day for 14 days) mounts a protective immune response to vaccinia virus infection in a lethal intranasal vaccinia virus challenge model of mice^[1].
Tecovirimat monohydrate (50 mg/kg, oral gavage, 5 days) can inhibit vaccinia virus-induced lesion formation following i.v. viral inoculation in Vaccinia virus-mouse tail lesion model^[1].
Tecovirimat monohydrate (100 mg/kg, p.o., daily for various durations of 5, 7, 10, or 14 days) significantly decreases in mortality of cowpox virus (CV)-infected mice^[2].

Pharmacokinetic parameters of ST-246 in mice^[1]

药代动力学分析^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

394.34

C₁₉H₁₇F₃N₂O₄

1162664-19-8

Solid

White to off-white

O=C(NN(C([C@]1([H])[C@@]2([H])[C@@](C3)([H])[C@@]3([H])[C@@](C=C2)([H])[C@]41[H])=O)C4=O)C5=CC=C(C(F)(F)F)C=C5.O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Quenelle DC, et al. Efficacy of delayed treatment with ST-246 given orally against systemic orthopoxvirus infections in mice[J]. Antimicrob Agents Chemother. 2007 Feb;51(2):689-95.  [Content Brief]

  [2]. DeLaurentis CE, et al. New Perspectives on Antimicrobial Agents: Tecovirimat monohydrate for Treatment of Human Monkeypox Virus[J]. Antimicrob Agents Chemother. 2022 Dec 20;66(12):e0122622.  [Content Brief]

  [3]. Yang G, et al. An orally bioavailable antipoxvirus compound (ST-246) inhibits extracellular virus formation and protects mice from lethal orthopoxvirus Challenge[J]. J Virol. 2005 Oct;79(20):13139-49.  [Content Brief]

  [4]. Russo AT, et al. An overview of Tecovirimat monohydrate for smallpox treatment and expanded anti-orthopoxvirus applications[J]. Expert Rev Anti Infect Ther. 2021 Mar;19(3):331-344.  [Content Brief]

  [5]. TYAVANAGIMATT SR, et al., Rehydration of micronized tecovirimat monohydrate. WO2015077143.

  [6]. Almehmadi M, et al. A Glance at the Development and Patent Literature of Tecovirimat monohydrate: The First-in-Class Therapy for Emerging Monkeypox Outbreak[J]. Viruses. 2022 Aug 25;14(9):1870.  [Content Brief]