| 产品描述： | Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology |
| 靶点： |
Oligomeric aggregates are presumed to be the key neurotoxic agent. Emrusolmin 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. Emrusolmin strongly inhibits all prion strains tested including BSE-derived and human prions. Emrusolmin shows structure-dependent binding to pathological aggregates and strongly inhibits formation of pathological oli |
| 体外研究： |
Emrusolmin shows structure-dependent binding to pathological aggregates and strongly inhibits formation of pathological oligomers in vitro and in vivo both for prion protein and α-synuclein. Emrusolmin (0.6-2 g/kg; p.o.) modulates α‐synuclein oligomerization. Animal Model: Two‐month‐old PLP‐hαSyn mice Dosage: 0.6 and 2 g/kg Administration: Oral Result: Prevented motor deficits and neurodegeneration in the PLP‐hαSyn mice. |
| 参考文献： |
1. Wagner J, et al. Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease. Acta Neuropathol. 2013 Jun;125(6):795-813. 2. Martinez Hernandez A, et al. The diphenylpyrazole compound anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology. EMBO Mol Med. 2018;10(1):32-47. 3. Heras-Garvin A, et al. Anle138b modulates α-synuclein oligomerization and prevents motor decline and neurodegeneration in a mouse model of multiple system atrophy. Mov Disord. 2019;34(2):255-263. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.914 ml |
14.57 ml |
29.14 ml |
| 5 mM |
0.583 ml |
2.914 ml |
5.828 ml |
| 10 mM |
0.291 ml |
1.457 ml |
2.914 ml |
| 50 mM |
0.058 ml |
0.291 ml |
0.583 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京