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Emrusolmin

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Chemical Structure| 882697-00-9 同义名 : Anle138b
CAS号 : 882697-00-9
货号 : A723997
分子式 : C16H11BrN2O2
纯度 : 99%+
分子量 : 343.175
MDL号 : MFCD30146410
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(145.7 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Anle138b ,the novel oligomer modulator, is an inhibitor of α-synuclein (α-syn) and prion-protein (PrPSc) aggregation that reduces the progression of prion and Parkinson′s disease in animal models. In vitro, anle138b blocked the formation of pathological aggregates of PrPSc and α-syn, which is deposited in PD and other synucleinopathies such as dementia with Lewy bodies (DLB) and multiple system atrophy (MSA). In mouse models of prion disease and PD mouse models, anle138b strongly inhibited oligomer accumulation, neuronal degeneration, and disease progression in vivo. [1] Anle138b is capable of prolonging the survival of prion-infected mice even after onset of symptoms, and anle138b started in the symptomatic disease phase at 50 weeks of life has a significant effect on survival until onset of terminal disease[2].Anle138b showed structure-dependent binding to pathological aggregates and strongly inhibited formation of pathological oligomers[1]. Anle138b strongly inhibited all prion strains including BSE-derived and human prions in a purely human system and had no detectable toxicity at therapeutic doses and an excellent oral bioavailability and blood–brain-barrier penetration , which indicated that this compound may also be useful for treatment of human prion disease[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.57mL

2.91mL

1.46mL

29.14mL

5.83mL

2.91mL

参考文献

[1]Wagner J, Ryazanov S, Leonov A, Levin J, Shi S, Schmidt F, Prix C, Pan-Montojo F, Bertsch U, Mitteregger-Kretzschmar G, Geissen M, Eiden M, Leidel F, Hirschberger T, Deeg AA, Krauth JJ, Zinth W, Tavan P, Pilger J, Zweckstetter M, Frank T, Bähr M, Weishaupt JH, Uhr M, Urlaub H, Teichmann U, Samwer M, Bötzel K, Groschup M, Kretzschmar H, Griesinger C, Giese A. 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. doi: 10.1007/s00401-013-1114-9. Epub 2013 Apr 19. PMID: 23604588; PMCID: PMC3661926.

[2]Levin J, Schmidt F, Boehm C, Prix C, Bötzel K, Ryazanov S, Leonov A, Griesinger C, Giese A. The oligomer modulator anle138b inhibits disease progression in a Parkinson mouse model even with treatment started after disease onset. Acta Neuropathol. 2014 May;127(5):779-80. doi: 10.1007/s00401-014-1265-3. Epub 2014 Mar 11. PMID: 24615514; PMCID: PMC3984662.