This product is discontinued due to commercial reason.
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1mg |
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5mg |
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Other Sizes |
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Purity: ≥98%
This product is discontinued due to commercial reason. Tecovirimat (formerly known as ST-246; SIGA-246; trade name: TPOXX), a p37 envelope protein inhibitor, is a small synthetic antiviral compound being developed to treat pathogenic orthopoxvirus infections of humans like smallbox. On 7/13/2018, FDA approved Tecovirimat for the treatment of smallbox infection. Tecovirimat was discovered as part of an HTS/high throughput screen program designed to identify inhibitors of vaccinia virus-induced cytopathic effects. The antiviral activity is specific for orthopoxviruses and the compound does not inhibit the replication of other RNA- and DNA-containing viruses or inhibit cell proliferation at concentrations of compound that are antiviral. Tecovirimat is an antiviral with activity against orthopoxviruses such as smallpox and is currently undergoing clinical trials. It works by blocking cellular transmission of the virus, thus preventing the disease.
References |
:N Engl J Med.2018 Nov 22;379(21):2084-2085;Viruses.2010 Nov;2(11):2409-35.
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Molecular Formula |
C19H15F3N2O3
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Molecular Weight |
376.35
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CAS # |
869572-92-9
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Related CAS # |
Tecovirimat-d4
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SMILES |
O=C(NN(C(C1C2C(C3)C3C(C=C2)C41)=O)C4=O)C5=CC=C(C(F)(F)F)C=C
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Chemical Name |
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.64 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6571 mL | 13.2855 mL | 26.5710 mL | |
5 mM | 0.5314 mL | 2.6571 mL | 5.3142 mL | |
10 mM | 0.2657 mL | 1.3286 mL | 2.6571 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Structure activity relationships and chemical information forST-246.Viruses.2010 Nov;2(11):2409-35. th> |
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ST-246inhibits production of extracellular virus and systemic virus spreadin vitroandin vivo.Viruses.2010 Nov;2(11):2409-35. td> |
Dose normalized exposure ofST-246in BALB/c mice from Day 1 of multiple studies.Viruses.2010 Nov;2(11):2409-35. td> |
Correlation between maximum monkeypox viral DNA levels in the bloodversusmaximum lesion number in non-human primates infected with monkeypox virus.Viruses.2010 Nov;2(11):2409-35. th> |
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Efficacy ofST-246in a non-human primate model of monkeypox virus infection.Viruses.2010 Nov;2(11):2409-35. td> |
A comparison ofST-246exposure (area under the concentration time curve, AUC) in monkeys and humans.Viruses.2010 Nov;2(11):2409-35. td> |