Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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ln Vitro |
In neural cells, LEI-401 decreases a variety of NAEs, including anandamide, in a way that is dependent on NAPE-PLD. With an IC50 of 0.86 μM, LEI-401 (0.04 – 20 μM; 30 min) dose-dependently decreased NAPE-PLD staining in hNAPE-transfected HEK293T cells. In Neuro-2a cells, LEI-401 lowers NAE levels, but not in NAPE-PLD KO cells [1].
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ln Vivo |
In mice, LEI-401 (30 mg/kg; i.p.) decreases fear extinction[1]. Moreover, HPA axis signaling is activated by LEI-401[1]. t1/2, Cmax, tmax, AUClast, and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively, were observed with LEI-401 (10 mg/kg; po) treatment[1]. Cmax, tmax, AUClast, and F values for LEI-401 (30 mg/kg; ip) dosing were 10,300 ng/mL, 1 hour, 38,600 h*ng/mL, and 48%, respectively[1].
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Animal Protocol |
Animal/Disease Models: Male 7–12weeks old C57BL/6J mice[1]
Doses: 30 mg/kg Route of Administration: Ip Experimental Results: Produced a significant increase in freezing as compared to vehicle. Animal/Disease Models: C57BL/6J mice[1] Doses: 10 mg/kg Route of Administration: Po (pharmacokinetic/PK Analysis) Experimental Results: The t1/2, Cmax, tmax, AUClast, and F values were 2.5 hrs (hours), 1370 ng/mL, 2 hrs (hours), 6760 h*ng/mL, and 25 %, respectively. |
References |
[1]. Mock ED, et al. Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice. Nat Chem Biol. 2020;16(6):667-675.
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Molecular Formula |
C24H31N5O2
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Molecular Weight |
421.54
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CAS # |
2393840-15-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
BrC1C=CC=CC=1N1C(C)=C(C(NC2C=CC3C=CC=CC=3N=2)=O)C=N1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 100 mg/mL (237.23 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.2372 mL | 1.1861 mL | 2.3723 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.