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Submit ReviewLEI 401
Description: High affinity N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) inhibitor
Chemical Name: N-(Cyclopropylmethyl)-6-[(3S)-3-hydroxy-1-pyrrolidinyl]-2-[(3S)-3-phenyl-1-piperidinyl]-4-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for LEI 401
LEI 401 is a high affinity N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) inhibitor (Ki = 0.027 and 0.18 μM for human and mouse NAPE-PLD, respectively; IC50 for human enzyme = 0.86 μM). LEI 401 exhibits no significant activity at cannabinoid receptors or other metabolic enzymes of the endocannabinoid system. The product reduces levels of N-acylethanolamines (NAE) in a neuroblastoma cell line in vitro. It also reduces anandamide levels in mouse brain in vivo and impairs fear extinction. LEI 701 is CNS penetrant and cell-permeable.
Licensing Information
Sold with kind permission of Professor van der Stelt
Compound Libraries for LEI 401
LEI 401 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LEI 401
| M. Wt | 421.55 |
| Formula | C24H31N5O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2393840-15-6 |
| PubChem ID | 145998143 |
| InChI Key | GFHJYPQZBBHOCC-UXHICEINSA-N |
| Smiles | O[C@H]1CCN(C2=NC(N3CCC[C@@H](C4=CC=CC=C4)C3)=NC(C(NCC5CC5)=O)=C2)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LEI 401
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.16 | 100 | |
| ethanol | 21.1 | 50 |
Preparing Stock Solutions for LEI 401
The following data is based on the product molecular weight 421.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.86 mL | 23.72 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets for LEI 401
References for LEI 401
References are publications that support the biological activity of the product.
Mock et al (2020) Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice. Nat.Chem.Biol. 16 667 PMID: 32393901
If you know of a relevant reference for LEI 401, please let us know.
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Keywords: LEI 401, LEI 401 supplier, LEI401, N-acylphosphatidylethanolamine, phospholipase, D, NAPEPLD, N-acylethanolamines, NAE, inhibitors, inhibits, high, affinity, brain, penetrant, cell, permeable, endocannabinoids, cannabinoids, Phospholipases, 7407, Tocris Bioscience
Citations for LEI 401
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