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Leucettine L41 

Cat. No. M27803
Leucettine L41  Structure
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Biological Activity

Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively). Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model.

Chemical Information
Molecular Weight 307.3
Formula C17H13N3O3
CAS Number 1112978-84-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] B Souchet, et al. J Prev Alzheimers Dis. Cerebral Phospho-Tau Acts Synergistically with Soluble Aβ42 Leading to Mild Cognitive Impairment in AAV-AD Rats

[2] Thu Lan Nguyen, et al. Dis Model Mech. Correction of cognitive deficits in mouse models of Down syndrome by a pharmacological inhibitor of DYRK1A

[3] Gaëlle Naert, et al. Eur Neuropsychopharmacol. Leucettine L41, a DYRK1A-preferential DYRKs/CLKs inhibitor, prevents memory impairments and neurotoxicity induced by oligomeric Aβ25-35 peptide administration in mice

[4] Xavier Fant, et al. Mol Pharmacol. cdc-like/dual-specificity tyrosine phosphorylation-regulated kinases inhibitor leucettine L41 induces mTOR-dependent autophagy: implication for Alzheimer's disease

[5] Guillaume Burgy, et al. Eur J Med Chem. Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines

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Keywords: Leucettine L41  supplier, CDK, inhibitors, activators


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