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Lemborexant

Chemical Structure : Lemborexant

CAS No.: 1369764-02-2

Lemborexant (E-2006, E2006)

Catalog No.: PC-45062Not For Human Use, Lab Use Only.

Lemborexant (E2006) is an orally active, potent, selective, dual Orexin receptor OX1/2 antagonist with binding Ki of 6/3 nM, respectively.

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Biological Activity

Lemborexant (E2006) is an orally active, potent, selective, dual Orexin receptor OX1/2 antagonist with binding Ki of 6/3 nM, respectively.
Lemborexant (E2006) exhibits an overall improvement in properties such as the TDI of CYP3A and aqueous solubility, high OXRs antagonist activity and sufficient brain penetration.
Lemborexant (E2006)  demonstrates high efficacy in preclinical sleep experiments.

Physicochemical Properties

M.Wt 410.4166
Formula C22H20F2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

Cyclopropanecarboxamide, 2-[[(2,4-dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)-, (1R,2S)-

References

1. Yoshida Y, et al. J Med Chem. 2015 Jun 11;58(11):4648-64.

2. Beuckmann CT, et al. J Pharmacol Exp Ther. 2017 Aug;362(2):287-295.

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