PF-07957472
Based on 1 Customer Validation
PF-07957472 (Compound 4) is an orally active and selective SARS-CoV-2 papain-like protease (PLpro) inhibitor, with a Ki of 2 nM against SARS-CoV-2 PLpro. PF-07957472 reduces SARS-CoV-2 viral titers in the lungs of infected mice and inhibits SARS-CoV-2-induced cytopathic effects in cells. PF-07957472 can be used for the research of COVID-19.
For research use only. We do not sell to patients.
- Purity: 99.13%
- CAS No.: 3041047-51-9
- Formula: C29H32N6O
- Molecular Weight:480.60
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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SARS-CoV-2 PLpro 2 |
PF-07957472 (serial dilutions; 30 min preincubation, 60 min reaction) potently inhibits purified recombinant SARS-CoV-2 PLpro with a Ki of 2 nM[1].
PF-07957472 (serial dilutions) inhibits SARS-CoV-2-induced CPE in Vero E6 cells (in the presence of 2 μM P-glycoprotein inhibitor CP-100356) with an EC50 of 147 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (8-week-old female)[1]
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Dosage:20 mg/kg; 50 mg/kg; 150 mg/kg
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Administration:oral; twice daily
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Result:Reduced lung viral titers to statistically significant levels at 50 and 150 mg/kg at 4 days post-infection.
Reduced viral levels to the limit of detection in half of the 150 mg/kg dose group mice.
Prevented infection-associated weight loss at all tested doses, whereas vehicle-treated infected mice showed ~10% body weight loss.
Chemical Information
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CAS No. 3041047-51-9
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Appearance Solid
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Molecular Weight 480.60
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Formula C29H32N6O
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Color Off-white to light brown
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SMILES
O=C(C1=CC(N2CCN(CC2)C)=CC=C1C)NC3(CC3)C4=C5C=CC=CC5=NC(C6=CN(C)N=C6)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (52.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 | 2.0807 mL | 10.4037 mL | 20.8073 mL | 52.0183 mL |
| 5 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL | 10.4037 mL | |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0807 mL | 5.2018 mL | |
| 15 mM | 0.1387 mL | 0.6936 mL | 1.3872 mL | 3.4679 mL | |
| 20 mM | 0.1040 mL | 0.5202 mL | 1.0404 mL | 2.6009 mL | |
| 25 mM | 0.0832 mL | 0.4161 mL | 0.8323 mL | 2.0807 mL | |
| 30 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7339 mL | |
| 40 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3005 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4161 mL | 1.0404 mL |
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