| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | 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 oligomers both for prion protein and α-synuclein[1]. | ||||||||||||
| In Vivo | 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[1]. Emrusolmin (0.6-2 g/kg; p.o.) modulates α‐synuclein oligomerization[3]. Animal Model: | ||||||||||||
| Name | Emrusolmin | ||||||||||||
| CAS | 882697-00-9 | ||||||||||||
| Formula | C16H11BrN2O2 | ||||||||||||
| Molar Mass | 343.17 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |
Emrusolmin
CAS: 882697-00-9 F: C16H11BrN2O2 W: 343.17
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion pro
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.