Referencia número: HY-14805

Tecovirimat

(Synonyms: ST-246)

1 Cited Publications

Revisión del cliente

Based on 1 publication(s) in Google Scholar

Tecovirimat (ST-246) is an orally bioavailable and selective compound against orthopoxviruses including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat 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.

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Pureza: 99.88%
No. CAS: 869572-92-9
Fòrmula: C₁₉H₁₅F₃N₂O₃
Peso molecular:376.33

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tecovirimat Chemical Structure

No. CAS: 869572-92-9

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Biosaf Health. 2025 Jan 5.

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Microbiological Assay

Microbiological Assay

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
HFF	CC₅₀	>100 μM Compound: ST-246	Cytotoxicity against HFF cells Cytotoxicity against HFF cells	[PMID: 17116683]
HFF	EC₅₀	0.05 μM Compound: ST-246	Antiviral activity against Vaccinia virus Copenhagen infected HFF cells Antiviral activity against Vaccinia virus Copenhagen infected HFF cells	[PMID: 17116683]
HFF	EC₅₀	0.1 μM Compound: ST-246	Antiviral activity against Vaccinia virus WR infected HFF cells Antiviral activity against Vaccinia virus WR infected HFF cells	[PMID: 17116683]
HFF	EC₅₀	0.48 μM Compound: ST-246	Antiviral activity against Cowpox virus Brighton infected HFF cells Antiviral activity against Cowpox virus Brighton infected HFF cells	[PMID: 17116683]
HFF	CC₅₀	>100 μM Compound: ST-246	Cytotoxicity against HFF cells after 7 days by neutral red assay Cytotoxicity against HFF cells after 7 days by neutral red assay	[PMID: 17724153]
HFF	EC₅₀	0.05 μM Compound: ST-246	Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction plaque formation after 3 days Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction plaque formation after 3 days	[PMID: 17724153]
HFF	EC₅₀	0.1 μM Compound: ST-246	Antiviral activity against Vaccinia virus WR in HFF cells assessed as reduction plaque formation after 3 days Antiviral activity against Vaccinia virus WR in HFF cells assessed as reduction plaque formation after 3 days	[PMID: 17724153]
HFF	EC₅₀	0.48 μM Compound: ST-246	Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction plaque formation after 3 days Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction plaque formation after 3 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Camelpox virus in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Camelpox virus in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Cowpox virus Brighton in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Cowpox virus Brighton in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Ectromelia virus Moscow in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Ectromelia virus Moscow in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Monkeypox virus in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Monkeypox virus in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
HFF	EC₅₀	≤0.07 μM Compound: ST-246	Antiviral activity against Variola virus in HFF cells assessed as inhibition of viral replication after 7 days Antiviral activity against Variola virus in HFF cells assessed as inhibition of viral replication after 7 days	[PMID: 17724153]
Vero	CC₅₀	>266 μM Compound: Tecovirimat	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by neutral red dye based colorimetric analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by neutral red dye based colorimetric analysis	[PMID: 33965861]

In Vitro

Tecovirimat (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.

Cell Cytotoxicity Assay^[1]

Cell Line:

Vero cells
Concentration:

0-50 μM
Incubation Time:

3 days
Result:

Was more potent relative to Cidofovir (CDV) (HY-17438) after vaccinia virus strain NYCBH infection in cytopathic effect (CPE)-based assays in vero cells.

In Vivo

Tecovirimat (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 (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 (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 Tecovirimat administered by oral gavage in mice^[1]

Dosage (mg/kg)	T_max (h)	C_max (μg/mL)	AUC_0-t (μg·h/mL)	T_1/2 (h)
30	2.7	32.5	284.2	2.5
100	1.0	62.2	287.6	2.5

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

Animal Model:

Weanling BALB/c mice challenged with vaccinia virus strain(4 to 6 weeks of age and weighing 15 to 20 g)^[1]
Dosage:

50 mg/kg
Administration:

oral gavage, twice a day for 14 days
Result:

Tecovirimat-treated mice mounted a protective immune response to vaccinia virus infection in a lethal intranasal vaccinia virus challenge model.

Animal Model:

NMRI mice inoculated via the tail vein with vaccinia virus(4 to 6 weeks of age and weighing 15 to 20 g)^[1]
Dosage:

50 mg/kg
Administration:

oral gavage, 5 days
Result:

Showed a dose-dependent reduction in the numbers of tail lesions at day 8 postinfection relative to placebo-treated control animals in mice.

Chemical Information

No. CAS 869572-92-9
Appearance Solid
Peso molecular 376.33
Fòrmula C₁₉H₁₅F₃N₂O₃
Color White to off-white
SMILES

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
Synonyms

ST-246
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Biosaf Health

2025 Jan 5.

Tecovirimat purchased from MedChemExpress. Usage Cited in: Biosaf Health. 2025 Jan 5.

Inhibition of EEV by ST-246 (Tecovirimat). HeLa cells were infected with VACV WR at a MOI of 3 for 2 h and then added increased dosages of ST-246 for another 22 h. The EEV was collected and titrated by BSC-1 cells.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (265.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6572 mL

13.2862 mL

26.5724 mL

5 mM

0.5314 mL

2.6572 mL

5.3145 mL

10 mM

0.2657 mL

1.3286 mL

2.6572 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.64 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

[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. [Content Brief]

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

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

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6572 mL	13.2862 mL	26.5724 mL	66.4311 mL
	5 mM	0.5314 mL	2.6572 mL	5.3145 mL	13.2862 mL
	10 mM	0.2657 mL	1.3286 mL	2.6572 mL	6.6431 mL
	15 mM	0.1771 mL	0.8857 mL	1.7715 mL	4.4287 mL
	20 mM	0.1329 mL	0.6643 mL	1.3286 mL	3.3216 mL
	25 mM	0.1063 mL	0.5314 mL	1.0629 mL	2.6572 mL
	30 mM	0.0886 mL	0.4429 mL	0.8857 mL	2.2144 mL
	40 mM	0.0664 mL	0.3322 mL	0.6643 mL	1.6608 mL
	50 mM	0.0531 mL	0.2657 mL	0.5314 mL	1.3286 mL
	60 mM	0.0443 mL	0.2214 mL	0.4429 mL	1.1072 mL
	80 mM	0.0332 mL	0.1661 mL	0.3322 mL	0.8304 mL
	100 mM	0.0266 mL	0.1329 mL	0.2657 mL	0.6643 mL

Keywords

Tecovirimat

1 Cited Publications

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Tecovirimat

Anti-Infection Compound Library

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Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

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High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tecovirimat

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Tecovirimat

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Anti-Orthopoxvirus Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tecovirimat

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Tecovirimat Related Classifications

Referencia número: HY-14805