Tecovirimat (Synonyms: ST-246)

Name: Tecovirimat
Brand: MedChemExpress
SKU: HY-14805
Rating: 4.5 (1 reviews)

Cat. No.: HY-14805 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Tecovirimat Chemical Structure

CAS No. : 869572-92-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
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	≤ 0.07 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 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 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 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]
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]
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.

Molecular Weight

376.33

Formula

C₁₉H₁₅F₃N₂O₃

CAS No.

869572-92-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Tecovirimat Related Classifications

Inflammation/Immunology Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tecovirimat869572-92-9ST-246ST246ST 246ArenavirusOrthopoxvirusorthopoxvirusesVP37antiviral activityF13Lorthopoxvirus-induced diseasesvero cellsInhibitorinhibitorinhibit

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Tecovirimat (Synonyms: ST-246)

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Complete Stock Solution Preparation Table

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