2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. LEI-401

LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.

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LEI-401 Chemical Structure

LEI-401 Chemical Structure

CAS No. : 2393840-15-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
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5 mg USD 150 In-stock
10 mg USD 220 In-stock
25 mg USD 450 In-stock
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100 mg USD 1350 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

LEI-401 Related Antibodies

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Phospholipase A PLD Phospholipase C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].

In Vitro

LEI-401 reduced a broad range of NAEs including anandamide in neuronal cells in a NAPE-PLD-dependent manner. LEI-401 (0.04-20 μM; 30?minutes) dose-dependently reduces the labeling of NAPE-PLD with an IC50 of 0.86 μM in hNAPE-PLD-transfected HEK293T cells. LEI-401 reduces NAE levels in Neuro-2a cells, but not in NAPE-PLD KO cells[1].

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

LEI-401 Related Antibodies
In Vivo

LEI-401 (30?mg/kg; i.p.) diminishes fear extinction in mice[1].
? LEI-401 also activates HPA axis signaling[1].
? LEI-401 (10 mg/kg; p.o.) treatment shows the t1/2, Cmax, tmax, AUClast, and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively[1].
? LEI-401 (30 mg/kg; i.p.) treatment show the Cmax, tmax, AUClast, and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively[1].

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

Animal Model: Male 7–12-week-old C57BL/6J mice[1]
Dosage: 30 mg/kg
Administration: I.p.
Result: Produced a significant increase in freezing as compared to vehicle.
Animal Model: C57BL/6J mice[1]
Dosage: 10 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: The t1/2, Cmax, tmax, AUClast, and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
Molecular Weight

421.54

Formula

C24H31N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC(N2C[C@H](C3=CC=CC=C3)CCC2)=NC(N4C[C@@H](O)CC4)=C1)NCC5CC5
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 (237.23 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 2.3723 mL 11.8613 mL 23.7225 mL
5 mM 0.4745 mL 2.3723 mL 4.7445 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.

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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:
%
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% 
+
%
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, 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 2.3723 mL 11.8613 mL 23.7225 mL 59.3064 mL
5 mM 0.4745 mL 2.3723 mL 4.7445 mL 11.8613 mL
10 mM 0.2372 mL 1.1861 mL 2.3723 mL 5.9306 mL
15 mM 0.1582 mL 0.7908 mL 1.5815 mL 3.9538 mL
20 mM 0.1186 mL 0.5931 mL 1.1861 mL 2.9653 mL
25 mM 0.0949 mL 0.4745 mL 0.9489 mL 2.3723 mL
30 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9769 mL
40 mM 0.0593 mL 0.2965 mL 0.5931 mL 1.4827 mL
50 mM 0.0474 mL 0.2372 mL 0.4745 mL 1.1861 mL
60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9884 mL
80 mM 0.0297 mL 0.1483 mL 0.2965 mL 0.7413 mL
100 mM 0.0237 mL 0.1186 mL 0.2372 mL 0.5931 mL
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LEI-401 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:

LEI-4012393840-15-6LEI401LEI 401PhospholipaseemotionalbehaviorCNSneuronalcellsHEK293Tbrain-penetrantHPAaxissignalingInhibitorinhibitorinhibit

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