Lemborexant (Synonyms: E-2006) |
| Catalog No.GC19220 |
Lemborexant(E2006)은 구강 투여용 활성 믹스티드 액티브 리세프터 앙태고니스트(DORA)이며, 불면증 치료를 위해 미국 식품의약국의 승인을 받았다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1369764-02-2
Sample solution is provided at 25 µL, 10mM.
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Lemborexant(E2006)은 구강 투여용 활성 믹스티드 액티브 리세프터 앙태고니스트(DORA)이며, 불면증 치료를 위해 미국 식품의약국의 승인을 받았다.
Lemborexant(1-25mg; 15일)는 수면 시작(LPS 감소)과 수면 유지(WASO 감소)를 개선하여 용량에 관련된 방식으로 수면 효율성(SE)에 긍정적인 영향을 미쳤다[2]. 62명의 참가자 중, 일주기 리듬에 따라 낮과 밤의 파라미터(placebo, n = 12; lemborexant 2.5 mg [LEM2.5], n = 12; lemborexant 5 mg [LEM5], n = 13, lemborexant 10 mg [LEM10], n = 13, lemborexant 15 mg [LEM15], n = 12). 평균 최소 활동 5시간(L5)은 기선에서 4주까지 LEM2.5, LEM5, LEM15는 placebo에 비해 현저하게 감소했으며, 이는 불안감의 감소를 시사한다[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.
| 동물 실험 [1]: | |
동물 모형 | 19세부터 80세까지의 남성과 여성 (불면증 환자) |
제조 방법 | 약은 취침 30분 전에 복용되었습니다. |
제형 | 1-25mg;15일 |
응용 분야 | Lemborexant는 수면 시작 시간(LPS 감소)과 수면 유지(WASO 감소)를 개선하여 수면 효율성(SE)에 긍정적인 영향을 미쳤으며 이는 용량과 관련이 있습니다. |
참고문헌: [1]. Murphy P, Moline M, Mayleben D, Rosenberg R, Zammit G, Pinner K, Dhadda S, Hong Q, Giorgi L, Satlin A. 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. | |
| Cas No. | 1369764-02-2 | SDF | |
| Synonyms | E-2006 | ||
| Canonical 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 | ||
| Formula | C22H20F2N4O2 | M.Wt | 410.42 |
| Solubility | DMSO : ≥ 30 mg/mL (73.10 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL |
| 5 mM | 487.3 μL | 2.4365 mL | 4.8731 mL |
| 10 mM | 243.7 μL | 1.2183 mL | 2.4365 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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