1. Metabolic Enzyme/Protease Others
  2. Endogenous Metabolite Amino Acid Derivatives
  3. Levacetylleucine

Levacetylleucine, an orally bioavailable and brain-penetrant endogenous metabolite, is an acetylated derivative of amino acid leucine. Levacetylleucine is the active form of N-acetyl-leucine (NAL). Levacetylleucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. Levacetylleucine also potentially improves ameliorates lysosomal and metabolic dysfunction. Levacetylleucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. Levacetylleucine is promising for research of neurological manifestations of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention.

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Levacetylleucine Chemical Structure

Levacetylleucine Chemical Structure

CAS No. : 1188-21-2

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Based on 1 publication(s) in Google Scholar

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Description

Levacetylleucine, an orally bioavailable and brain-penetrant endogenous metabolite, is an acetylated derivative of amino acid leucine. Levacetylleucine is the active form of N-acetyl-leucine (NAL). Levacetylleucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. Levacetylleucine also potentially improves ameliorates lysosomal and metabolic dysfunction. Levacetylleucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. Levacetylleucine is promising for research of neurological manifestations of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention[1][2][3][4].

IC50 & Target

Human Endogenous Metabolite

 

In Vivo

Levacetylleucine (60 mg/kg, i.v., administration on days 1, 2 and 3 for 15 days) decreases the postural imbalance scores and accelerates the course of postural compensation induced by UL in rats[3].
Levacetylleucine (100 mg/kg, oral gavage, administration daily for 28 days) attenuates cortical cell death afer traumatic brain injury (TBI) in N-Acetyl-L-leucine-treated TBI mouse cortices[4].

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

Animal Model: Male Sprague-Dawley rats (mean 400±20 g, age 3 months) after chemical UL[3]
Dosage: 60 mg/kg
Administration: i.v., 15 days
Result: Significantly decreased the postural imbalance scores on 7 day and accelerated the course of postural compensation by about 6 days in rats.
Animal Model: C57/BL6 mice[4]
Dosage: 100 mg/kg
Administration: oral gavage, administration daily for 1-28 days
Result: Did not afect food intake and body weight in mice.
Animal Model: N-Acetyl-L-leucine-treated TBI mouse cortices[4]
Dosage: 100 mg/kg
Administration: oral gavage, administration daily for 28 days
Result: Prevented cortical cell death which peaks at early time points (day 1) afer TBI in N-Acetyl-L-leucine-treated TBI mouse cortices.
Molecular Weight

173.21

Formula

C8H15NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)C[C@H](NC(C)=O)C(O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (577.33 mM; Need ultrasonic; 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 5.7733 mL 28.8667 mL 57.7334 mL
5 mM 1.1547 mL 5.7733 mL 11.5467 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (14.43 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 (14.43 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:

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Dosing volume
(per animal)

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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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.7733 mL 28.8667 mL 57.7334 mL 144.3335 mL
5 mM 1.1547 mL 5.7733 mL 11.5467 mL 28.8667 mL
10 mM 0.5773 mL 2.8867 mL 5.7733 mL 14.4333 mL
15 mM 0.3849 mL 1.9244 mL 3.8489 mL 9.6222 mL
20 mM 0.2887 mL 1.4433 mL 2.8867 mL 7.2167 mL
25 mM 0.2309 mL 1.1547 mL 2.3093 mL 5.7733 mL
30 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8111 mL
40 mM 0.1443 mL 0.7217 mL 1.4433 mL 3.6083 mL
50 mM 0.1155 mL 0.5773 mL 1.1547 mL 2.8867 mL
60 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4056 mL
80 mM 0.0722 mL 0.3608 mL 0.7217 mL 1.8042 mL
100 mM 0.0577 mL 0.2887 mL 0.5773 mL 1.4433 mL
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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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Levacetylleucine
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