[CAS NO. 103476-89-7] Leupeptinhemisulfate

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PRODUCTS SPECIFICATIONS [103476-89-7]

Catalog

HY-18234A

Brand

MCE

CAS

103476-89-7

DESCRIPTION [103476-89-7]

Overview

MDL	MFCD00037012
Molecular Weight	475.59
Molecular Formula	C20H38N6O4.1/2H2SO4
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]

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

18 Publications Citing Use of MCE

Summary

Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor . Leupeptin hemisulfate potently inhibits serine , cysteine and threonine proteases . Leupeptin hemisulfate inhibits M ^pro (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 EC ₅₀ value of 42.34 µM ^[1] .
Leupeptin hemisulfate has some inhibitory activity against M ^pro , with an IC ₅₀ value of 127.2 µM ^[1] .
Leupeptin hemisulfate againsts human coronavirus strain 229E with an IC ₅₀ value of 0.4 µg/mL (about 1 µM) ^[1] .

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] .

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.

Appearance

Solid

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:

H ₂ O : 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
10 mM	0.2103 mL	1.0513 mL	2.1027 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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

* All of the co-solvents are available by MCE.

References

Synonyms

L-Leucinamide, N-acetyl-L-leucyl-N-[(1S)-4-[(aminoiminomethyl)amino]-1-formylbutyl]-, sulfate (2:1)

L-Leucinamide, N-acetyl-L-leucyl-N-[4-[(aminoiminomethyl)amino]-1-formylbutyl]-, (S)-, sulfate (2:1)

Leupeptin hemisulfate