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Lemborexant (Synonyms: E-2006)

رقم الكتالوجGC19220

Lemborexant (E-2006) هو مضاد مزدوج عكسي وتنافسي ونشط فمويًا لمستقبلات orexin OX1 و OX2 بقيم IC50 تبلغ 6.1 نانومتر و 2.6 نانومتر ، على التوالي

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Lemborexant التركيب الكيميائي

Cas No.: 1369764-02-2

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
257٫00
متوفر
5mg
234٫00
متوفر
10mg
405٫00
متوفر
25mg
720٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

Lemborexant (E2006) is an oral active diorexin receptor antagonist (DORA) and has been approved by the US Food and Drug Administration for the treatment of insomnia[1-2].

Lemborexant(1-25mg;15days) had a positive effect on Sleep Efficiency (SE) by improving both sleep onset (decreasing LPS) and sleep maintenance (decreasing WASO) in a dose-related manner[2]. In 62 subjects, according to circadian rhythm, day and night parameters (placebo, n = 12; lemborexant 2.5 mg [LEM2.5], n = 12; lemborexant 5 mg [LEM5], n = 13, lemborexant 10 mg [LEM10], n = 13 and lemborexant 15 mg [LEM15], n = 12). Mean least active 5 hours (L5) showed a decrease from baseline to week 4 for LEM2.5, LEM5 and LEM15 that was significantly greater than with placebo, suggesting a reduction in restlessness[3].

References:
[1]. Dayvigo [prescribing information] (lemborexant), Woodcliff Lake, NJ: Eisai Inc. US. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf. Accessed January 08, 2020.
[2]. Murphy P, Moline M, et,al. Lemborexant, A Dual Orexin Receptor Antagonist (DORA) for the Treatment of Insomnia Disorder: Results From a Bayesian, Adaptive, Randomized, Double-Blind, Placebo-Controlled Study. J Clin Sleep Med. 2017 Nov 15;13(11):1289-1299. doi: 10.5664/jcsm.6800. PMID: 29065953; PMCID: PMC5656478.
[3]. Moline M, Thein S, et,al. Safety and Efficacy of Lemborexant in Patients With Irregular Sleep-Wake Rhythm Disorder and Alzheimer's Disease Dementia: Results From a Phase 2 Randomized Clinical Trial. J Prev Alzheimers Dis. 2021;8(1):7-18. doi: 10.14283/jpad.2020.69. PMID: 33336219.

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