Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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Targets |
IC50: 53 nM (Mpro)[1]
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ln Vitro |
Bofutrelvir (24 hours) demonstrates in vitro action against SARS-CoV-2 and its variations, with EC50 values for SARS-CoV-2, SARS-CoV-2 (Alpha), SARS-CoV-2 (Beta), SARS-CoV-2 (Delta), and SARS-CoV-2 (Omicron) respectively of 0.42, 0.39, 0.28, 0.27, and 0.26 μM[2]. In vero E6 cells, bofutrelvir suppresses SARS-CoV-2 replication even at EC50 values when human blood is present (1.1–2.4 μM)[2]. In vitro, bofutrelvir and remdesivi therapy together show an additive impact against SARS-CoV-2[2].
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ln Vivo |
Effective against SARS-CoV-2 delta variant infection in vivo is bofutrelvir (100 and 200 mg/kg; ip once daily on day 0 and twice daily on days 1, 2, and 3 for 4 consecutive days)[2].
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Animal Protocol |
Animal/Disease Models: K18-hACE2 mice with SARS-CoV-2 delta variant infection[2]
Doses: 100 and 200 mg/kg Route of Administration: intraperitoneal (ip)injection; 100 and 200 mg/ kg one time/day on day 0 and twice (two times) daily on day 1, 2 and 3 for 4 days Experimental Results: demonstrated a dose-dependent efficacy to virus titers of lung. Effectively reduces the lung viral loads. Dose-dependently demonstrated antiviral activity against the SARS -CoV-2 Delta variant and Dramatically diminished viral load in mouse lung and brain. |
References |
[1]. Ullrich S, Nitsche C. The SARS-CoV-2 main protease as drug target. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127377.
[2]. Shang W, et al. In vitro and in vivo evaluation of the main protease inhibitor FB2001 against SARS-CoV-2. Antiviral Res. 2022 Dec;208:105450. |
Molecular Formula |
C25H32N4O4
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Molecular Weight |
452.55
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CAS # |
2103278-86-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C([C@H](CC1CCCCC1)NC(C1=CC2C=CC=CC=2N1)=O)N[C@H](C=O)C[C@H]1C(NCC1)=O
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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) |
DMSO : 100 mg/mL (220.97 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 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 (5.52 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2097 mL | 11.0485 mL | 22.0970 mL | |
5 mM | 0.4419 mL | 2.2097 mL | 4.4194 mL | |
10 mM | 0.2210 mL | 1.1049 mL | 2.2097 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.