2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Oligomeric aggregates are presumed to be the key neurotoxic agent. Anle138b blocksthe formation of pathological aggregates of prion protein and of α-synuclein, which is deposited in Parkinson’s disease and other synucleinopathies such as dementia with Lewy bodies and multiple system atrophy. Anle138b strongly inhibits all prion strains tested including BSE-derived and human prions. Anle138b shows structure-dependent binding to pathological aggregates and strongly inhibits formation of pathological oligomers both for prion protein and α-synuclein.Anle138b has no detectable toxicity at therapeutic doses and an excellent oral bioavailability and blood–brain-barrier penetration. In mouse models of prion disease and in three different PD mouse models, anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression. Di-phenyl-pyrazole anle138b binds to aggregated tau and inhibits tau aggregation. Anle138b treatment effectively ameliorates disease symptoms, increases survival time and improves cognition of tau transgenic PS19 mice.
