1. Metabolic Enzyme/Protease Anti-infection
  2. Cathepsin Ser/Thr Protease Virus Protease
  3. Leupeptin hemisulfate

Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.

For research use only. We do not sell to patients.

Leupeptin hemisulfate Chemical Structure

Leupeptin hemisulfate Chemical Structure

CAS No. : 103476-89-7

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Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
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Solid
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10 mg USD 84 In-stock
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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of Leupeptin hemisulfate:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].

IC50 & Target

Cathepsin B, Cathepsin H, Cathepsin L, Ser/Thr Protease, Mpro[1][2][3].

In Vitro

Leupeptin hemisulfate (0.06-200 µM; 72 h) significantly decreases copy numbers of SARS-CoV-2 viral RNA (vRNA) in Vero cells[1]
Leupeptin hemisulfate inhibits RNA levels of SARS-CoV-2 in Vero cells, with an EC50 value of 42.34 µM[1].
Leupeptin hemisulfate has some inhibitory activity against Mpro, with an IC50 value of 127.2 µM[1].
Leupeptin hemisulfate againsts human coronavirus strain 229E with an IC50 value of 0.4 µg/mL (about 1 µM)[1].

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

RT-PCR[1]

Cell Line: Vero cells
Concentration: 0.06-200 µM
Incubation Time: 72 h
Result: Significantly decreased copy numbers of SARS-CoV-2 viral RNA (vRNA).
In Vivo

Leupeptin hemisulfate (0, 9, 18, 36 mg/kg; i.p.; single) is well tolerated by the animals and produces a strong, dose-dependent increase in LC3b-II in both the total tissue extracts and the lysosome and autophagosome-enriched pellet fraction[2].

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

Animal Model: C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)[1]
Dosage: 0, 9, 18, 36 mg/kg
Administration: Intraperitoneal injection; single
Result: Promoted the accumulation of LC3b-II in mouse liver.
Molecular Weight

475.59

Formula

C20H38N6O4.1/2H2SO4

CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

Ac-LLR-CHO

SMILES

O=C[C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N.[0.5H2SO4]

Structure Classification
Initial Source

Microbial Metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 83.33 mg/mL (175.21 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1027 mL 10.5133 mL 21.0265 mL
5 mM 0.4205 mL 2.1027 mL 4.2053 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (210.27 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

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 (sealed storage, away from moisture). 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
H2O 1 mM 2.1027 mL 10.5133 mL 21.0265 mL 52.5663 mL
5 mM 0.4205 mL 2.1027 mL 4.2053 mL 10.5133 mL
10 mM 0.2103 mL 1.0513 mL 2.1027 mL 5.2566 mL
15 mM 0.1402 mL 0.7009 mL 1.4018 mL 3.5044 mL
20 mM 0.1051 mL 0.5257 mL 1.0513 mL 2.6283 mL
25 mM 0.0841 mL 0.4205 mL 0.8411 mL 2.1027 mL
30 mM 0.0701 mL 0.3504 mL 0.7009 mL 1.7522 mL
40 mM 0.0526 mL 0.2628 mL 0.5257 mL 1.3142 mL
50 mM 0.0421 mL 0.2103 mL 0.4205 mL 1.0513 mL
60 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8761 mL
80 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6571 mL
100 mM 0.0210 mL 0.1051 mL 0.2103 mL 0.5257 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Leupeptin hemisulfate 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.

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Leupeptin hemisulfate
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