Emrusolmin  (Synonyms: Anle138b)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

343.17

Solid

C₁₆H₁₁BrN₂O₂

882697-00-9

BrC1=CC(C2=CC(C3=CC=C(OCO4)C4=C3)=NN2)=CC=C1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]