Elenbecestat (Synonyms: E2609)
目录号: PL13299 纯度: ≥99%
CAS No. :1388651-30-6
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中文名称
Elenbecestat
英文名称
Elenbecestat
英文别名
Elenbecestat;RXJ96XL94H;E2609;Elenbecestat [INN];Elenbecestat [USAN];Elenbecestat; E2609;Elenbecestat [USAN:INN];GTPL9818;s8600;DB15391;E 2609;D11509;N-[3-[(4aS,5R,7aS)-2-amino-5-methyl-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-(difluoromethyl)pyrazine-2-carboxamide;N-(3-((4aS,5R,7aS)-2-Amino-5-methyl-4a,5-dihydro-4H-furo(3,4-d)(1,3)thiazin-7a(7H)-yl)-4-fluorophenyl)-5-(difluo
Cas No.
1388651-30-6
分子式
C19H18F3N5O2S
分子量
437.44
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Elenbecestat (E2609) 是一种高效、有口服活性的,能透过 CNS 的 BACE-1 抑制剂。Elenbecestat 有潜力用于阿尔茨海默病 (AD) 的研究。
生物活性
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimers disease (AD) research.
性状
Solid
IC50 & Target[1][2]
BACE-1
体外研究(In Vitro)
Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay.
Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates.
Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Kumar D, et al.Secretase inhibitors for the treatment of Alzheimers disease: Long road ahead. Eur J Med Chem. 2018 Mar 25;148:436-452.
[2]. A single dose of the beta-secretase inhibitor, e2609, decreases CSF bace1 enzymatic activity in cynomolgus monkeys. Alzheimer’s & Dementia, 8(4), P224.
溶解度数据
In Vitro: DMSO : ≥ 250 mg/mL (571.51 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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