Art. -Nr.: HY-137048

PF-00835231

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

PF-00835231 is a CoV-2 cysteine 3C-like protease (3CL^pro) inhibitor, with IC₅₀s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CL^pro, respectively. PF-00835231 is developed for the research of anti-SARS-CoV-2/COVID-19. PF-00835231 can inhibit cell infections and also suppress infections in animal models.

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Reinheit: 99.31%
CAS. Nr.: 870153-29-0
Formel: C₂₄H₃₂N₄O₆
Molecular Weight:472.53

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-00835231 Chemical Structure

CAS. Nr.: 870153-29-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HIV-1

HRV3C

2.79 μM (IC₅₀)

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
H1-HeLa	CC₅₀	>1260 μM Compound: 4; PF-00835231	Cytotoxicity against human H1-HeLa cells assessed as reduction in cell viability measured after 2 to 5 days by XTT assay Cytotoxicity against human H1-HeLa cells assessed as reduction in cell viability measured after 2 to 5 days by XTT assay	[PMID: 33054210]
H9	CC₅₀	>32 μM Compound: 4; PF-00835231	Cytotoxicity against human H9 cells assessed as reduction in cell viability incubated for 7 days by XTT dye based analysis Cytotoxicity against human H9 cells assessed as reduction in cell viability incubated for 7 days by XTT dye based analysis	[PMID: 33054210]
HEK-293T	CC₅₀	>50000 nM Compound: PF-00835231	Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability	[PMID: 36229406]
Huh-7	CC₅₀	>320 μM Compound: 4; PF-00835231	Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability	[PMID: 33054210]
MRC5	CC₅₀	>100 μM Compound: 4; PF-00835231	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 1 to 5 days by XTT dye based assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 1 to 5 days by XTT dye based assay	[PMID: 33054210]
MRC5	CC₅₀	>40 μM Compound: 4; PF-00835231	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 4 days by XTT dye based assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 4 days by XTT dye based assay	[PMID: 33054210]
Vero 76	CC₅₀	452 μM Compound: 4; PF-00835231	Cytotoxicity against African green monkey Vero 76 cells measured after 66 hrs by neutral red method or cell titer glo-based luminescence assay Cytotoxicity against African green monkey Vero 76 cells measured after 66 hrs by neutral red method or cell titer glo-based luminescence assay	[PMID: 33054210]
Vero C1008	CC₅₀	>50000 nM Compound: PF-00835231	Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability	[PMID: 36229406]
Vero C1008	EC₅₀	0.23 μM Compound: PF-00835231	Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days	[PMID: 36475694]
Vero C1008	EC₅₀	21.7 nM Compound: PF-00835231	Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect	[PMID: 37229831]

In Vitro

PF-00835231 effectively inhibits SARS-CoV-2 USA-WA1/2020, with an EC₅₀ of 0.221 μM after 24 hours and 0.158 μM after 48 hours^[2].
PF-00835231 also inhibits USA/NYU-VC-003/2020, with an EC₅₀ of 0.184 μM after 24 hours^[2].
The IC₅₀ value of PF-00835231 against HIV-1 and HCV protease is greater than 10 μM, but it can inhibit the rhinovirus HRV3C protease with an IC₅₀ of about 2.79 μM, showing strong inhibitory effects and broad-spectrum activity against coronavirus Mp^[3].
PF-00835231 exhibits inhibitory effects against infections of the SARS-CoV-2 Wuhan strain, Washington strain 1, and Belgium/GHB-03021/2020 strain in A549, Calu-1, Vero E6, Vero E6-enACE2 (ACE2-rich Vero E6 kidney cells), and Vero E6-EGFP (Vero E6 cells continuously expressing EGFP), with EC₅₀ values ranging from 24.7 nM to 88900 nM^[3].

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

In Vivo

PF-00835231 reduces the number of multifocal lung lesions and lung viral load in the SARS-CoV-MA15 infected BALB/c mouse model, being effective both early and late in the viral infection^[3].

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

Chemical Information

CAS. Nr. 870153-29-0
Appearance Solid
Molecular Weight 472.53
Formel C₂₄H₃₂N₄O₆
Color White to off-white
SMILES

O=C(C(N1)=CC2=C1C=CC=C2OC)N[C@H](C(N[C@@H](C[C@H]3C(NCC3)=O)C(CO)=O)=O)CC(C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Virol Sin

The SARS-CoV-2 3CL protease inhibits pyroptosis through the cleavage of gasdermin D. [Abstract]

2025 Mar 19:S1995-820X(25)00028-8. PMID: 40118151
J Virol

Adaptive Mutation in the Main Protease Cleavage Site of Feline Coronavirus Renders the Virus More Resistant to Main Protease Inhibitors. [Abstract]

2022 Sep 14;96(17):e0090722. PMID: 36000844
Adv Biol (Weinh)

Predicting Clinical Outcomes of SARS-CoV-2 Drug Efficacy with a High-Throughput Human Airway Microphysiological System. [Abstract]

2024 Nov;8(11):e2300511. PMID: 39123296
bioRxiv

2025 Nov 17.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (529.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1163 mL

10.5813 mL

21.1627 mL

5 mM

0.4233 mL

2.1163 mL

4.2325 mL

10 mM

0.2116 mL

1.0581 mL

2.1163 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Robert L Hoffman, et al. Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. J Med Chem. 2020 Nov 12;63(21):12725-12747. [Content Brief]

[2]. de Vries M, et al. A comparative analysis of SARS-CoV-2 antivirals in human airway models characterizes 3CLpro inhibitor PF-00835231 as a potential new treatment for COVID-19. bioRxiv [Preprint]. 2021 Feb 19:2020.08.28.272880. [Content Brief]

[3]. Wujun Chen, wt al. Review of preclinical data of PF-07304814 and its active metabolite derivatives against SARS-CoV-2 infection. Front Pharmacol. 2022 Nov 11:13:1035969. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.1163 mL	10.5813 mL	21.1627 mL	52.9067 mL
	5 mM	0.4233 mL	2.1163 mL	4.2325 mL	10.5813 mL
	10 mM	0.2116 mL	1.0581 mL	2.1163 mL	5.2907 mL
	15 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5271 mL
	20 mM	0.1058 mL	0.5291 mL	1.0581 mL	2.6453 mL
	25 mM	0.0847 mL	0.4233 mL	0.8465 mL	2.1163 mL
	30 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7636 mL
	40 mM	0.0529 mL	0.2645 mL	0.5291 mL	1.3227 mL
	50 mM	0.0423 mL	0.2116 mL	0.4233 mL	1.0581 mL
	60 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	80 mM	0.0265 mL	0.1323 mL	0.2645 mL	0.6613 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5291 mL

Keywords

PF-00835231

4 Cited Publications

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PF-00835231

Anti-Hepatitis C Virus Compound Library

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Antiviral Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-00835231

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-00835231

Anti-Hepatitis C Virus Compound Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Antiviral Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-00835231

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-00835231 Related Classifications

HY-137048 Related Classifications