Tecovirimat (monohydrate)


CAS No. : 1162664-19-8

(Synonyms: ST-246 (monohydrate))

1162664-19-8
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Cat. No. : HY-14805A
M.Wt: 394.34
Formula: C19H17F3N2O4
Purity: >98 %
Solubility:
Introduction of 1162664-19-8 :

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].
In Vitro: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].
In Vivo: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]
Dosage (mg/kg) Tmax (h) Cmax (μg/mL) AUC0-t (μg·h/mL) T1/2 (h)
30 2.7 32.5 284.2 2.5
100 1.0 62.2 287.6 2.5

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