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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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L647223-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $150.90 | |
L647223-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $220.90 | |
L647223-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $450.90 | |
L647223-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $770.90 | |
L647223-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,350.90 |
Specifications & Purity | 99% |
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Storage Temp | Store at -20°C |
Shipped In | Dry ice |
Product Description | LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC 50 of 27 nM. LEI-401 modulates emotional behavior in mice. 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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LEI-401 (30 mg/kg; i.p.) diminishes fear extinction in mice . LEI-401 also activates HPA axis signaling . LEI-401 (10 mg/kg; p.o.) treatment shows the t 1/2 , C max , t max , AUC last , and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively . LEI-401 (30 mg/kg; i.p.) treatment show the C max , t max , AUC last , and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively . 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 Dosage: 30 mg/kg Administration: I.p. Result: Produced a significant increase in freezing as compared to vehicle. Animal Model: C57BL/6J mice Dosage: 10 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The t 1/2 , C max , t max , AUC last , and F values were 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively. Form:Solid |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | N-(cyclopropylmethyl)-6-[(3S)-3-hydroxypyrrolidin-1-yl]-2-[(3S)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide |
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INCHI | InChI=1S/C24H31N5O2/c30-20-10-12-28(16-20)22-13-21(23(31)25-14-17-8-9-17)26-24(27-22)29-11-4-7-19(15-29)18-5-2-1-3-6-18/h1-3,5-6,13,17,19-20,30H,4,7-12,14-16H2,(H,25,31)/t19-,20+/m1/s1 |
InChi Key | GFHJYPQZBBHOCC-UXHICEINSA-N |
Canonical SMILES | C1CC(CN(C1)C2=NC(=CC(=N2)N3CCC(C3)O)C(=O)NCC4CC4)C5=CC=CC=C5 |
Isomeric SMILES | C1C[C@H](CN(C1)C2=NC(=CC(=N2)N3CC[C@@H](C3)O)C(=O)NCC4CC4)C5=CC=CC=C5 |
PubChem CID | 145998143 |
Molecular Weight | 421.54 |
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Solubility | DMSO : 100 mg/mL (237.23 mM; Need ultrasonic) |
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