2. Anti-infection
  3. SARS-CoV Virus Protease
  4. PF-07957472

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.

PF-07957472

PF-07957472 Chemical Structure

CAS No. : 3041047-51-9

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PF-07957472 Related Antibodies

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Description

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[1].

IC50 & Target[1]

SARS-CoV-2 PLpro

2 <br/> nM (Ki)

In Vitro

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.

PF-07957472 Related Antibodies
In Vivo

PF-07957472 (20-150 mg/kg; p.o.; twice daily) causes a statistically significant reduction in SARS-CoV-2 lung viral titers in infected BALB/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (8-week-old female)[1]
Dosage: 20 mg/kg; 50 mg/kg; 150 mg/kg
Administration: oral; twice daily
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.
Molecular Weight

480.60

Formula

C29H32N6O
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(C1=CC(N2CCN(CC2)C)=CC=C1C)NC3(CC3)C4=C5C=CC=CC5=NC(C6=CN(C)N=C6)=C4
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 : 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0807 mL 10.4037 mL 20.8073 mL
5 mM 0.4161 mL 2.0807 mL 4.1615 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 (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.
  • Protocol 2

    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.
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
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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PF-07957472 Related Classifications

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:

PF-079574723041047-51-9PF07957472PF 07957472SARS-CoVVirus ProteaseSARS coronavirusSARS-CoV-2 papain-like proteasemouse lungsMERS coronaviruses PLprodNHBE cellsSARS-CoV PLproVero E6 cellsBALB/c mice229E coronaviruses PLproSARS-CoV-2 PLproOC43 coronaviruses PLproInhibitorinhibitorinhibit

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