1. Anti-infection
  2. Arenavirus Orthopoxvirus
  3. Tecovirimat

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

Tecovirimat Chemical Structure

CAS No. : 869572-92-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 400 In-stock
25 mg USD 780 In-stock
50 mg USD 1345 In-stock
100 mg USD 1880 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tecovirimat:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5].

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) 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

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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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)

g

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%

References

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.

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
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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.

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