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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-Lemborexant
Lemborexant

Chemical Structure : Lemborexant

CAS No.: 1369764-02-2

Lemborexant (E-2006, E2006)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 410.4166
分子式 C22H20F2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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)-

参考文献

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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