您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Anle138b
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Anle138b
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Anle138b图片
CAS NO:882697-00-9
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
Anle138b 是一种毒性低,口服生物利用度高,血脑屏障通透性好的低聚物聚集抑调节剂,可阻断朊病毒蛋白和 α-突触核蛋白病理性聚集的形成。它在体内强烈抑制低聚物积累、神经元变性和疾病进展。它阻断 Aβ 通道并挽救淀粉样变性小鼠模型的疾病表型。

产品描述

Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease

体外活性

In vitro, anle138b blocked the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn), which is deposited in PD and other synucleinopathies such as dementia with Lewy bodies (DLB) and multiple system atrophy (MSA).

体内活性

Anle138b strongly inhibited all prion strains tested including BSE-derived and human prions.?Anle138b showed structure-dependent binding to pathological aggregates and strongly inhibited formation of pathological oligomers in vitro and in vivo both for prion protein and α-synuclein.?Both in mouse models of prion disease and in three different PD mouse models, anle138b strongly inhibited oligomer accumulation, neuronal degeneration, and disease progression in vivo.?Anle138b had no detectable toxicity at therapeutic doses and an excellent oral bioavailability and blood-brain-barrier penetration.

动物实验

anle138b was administered orally in DMSO/peanut butter as described above.?In a first set of experiments, 5 mg anle138b were given once daily starting either at day 80 or day 120 post i.c. infection.?Animals of each treatment group were monitored daily for signs of disease by trained animal caretakers from day 80 post infection.?The animals were sacrificed, when they had reached the terminal stage of the disease based on clinical signs (ataxia, tremor, difficulty in righting up from a position lying on its back and tail stiffness).?Typically the disease progress through the terminal stage will lead to the death of the animal within 1 or 2 days.?In addition, groups of four mice per experimental group were sacrificed at predefined time points. From all animals, one brain hemisphere and one half of the spleen were freshly frozen at 80 C for biochemical analysis.?The other hemisphere and the remaining half of the spleen as well as all inner organs were fixed in 4 % formaldehyde solution for histological analysis.?In a further experiment, treatment with anle138b was started on the day of i.c. infection with a dose of 5 mg anle138b twice daily.

Cas No.

882697-00-9

分子式

C16H11BrN2O2

分子量

343.18

储存和溶解度

DMSO:50 mg/mL (145.70 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years