Lemborexant( E-2006 | E2006 )

Catalog No. M11522 CAS No. 1369764-02-2

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Product Name

Lemborexant
Note

Research use only, not for human use.
Brief Description

An orally active, potent, selective, dual Orexin receptor OX1/2 antagonist with binding Ki of 6/3 nM, respectively.
Description

An orally active, potent, selective, dual Orexin receptor OX1/2 antagonist with binding Ki of 6/3 nM, respectively; exhibits an overall improvement in properties such as the TDI of CYP3A and aqueous solubility, high OXRs antagonist activity and sufficient brain penetration; demonstrates high efficacy in preclinical sleep experiments.Sleep Disorder Phase 3 Clinical.
In Vitro

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In Vivo

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Synonyms

E-2006 | E2006
Pathway

GPCR/G Protein
Target

Orexin Receptor
Recptor

Orexin Receptor
Research Area

Neurological Disease
Indication

Sleep Disorder

CAS Number

1369764-02-2
Formula Weight

410.4166
Molecular Formula

C22H20F2N4O2
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 30 mg/mL
SMILES

O=C([C@H]1[C@@](C2=CC=CC(F)=C2)(COC3=CN=C(C)N=C3C)C1)NC4=NC=C(F)C=C4
Chemical Name

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

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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