Anle138b

An inhibitor of protein aggregation

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库存: 现货

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5mg

￥700.00

560.00

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10mg

￥1200.00

960.00

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25mg

￥2587.00

2070.00

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50mg

￥4487.00

3590.00

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100mg

￥7912.00

6330.00

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200mg

￥13775.00

11020.00

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货号: ajce45934
CAS: 882697-00-9
别名: 3-(1,3-苯并二恶唑-5-基)-5-(3-溴苯基)-1H-吡唑
分子式: C16H11BrN2O2
分子量: 343.17
纯度: >98%
溶解度: DMSO : ≥ 50 mg/mL (145.70 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Anle138b is an inhibitor of protein aggregation.¹ It inhibits α-synuclein oligomer formation and PrP^Sc prion propagation by 77 and 84%, respectively, when used at a concentration of 10 ?M. Anle138b (1 mg/animal) inhibits brain accumulation of PrP^Sc in, and increases survival of, prion-infected mice. It reduces brain tau deposition and rescues glucose metabolic decline in a human tau transgenic mouse model of Alzheimer’s disease.² Dietary administration of anle138b (0.6 and 2 g/kg chow) reduces the formation of α-synuclein oligomers and glial cytoplasmic inclusions, microglial activation, and dopaminergic neuron degradation, as well as preserves motor function, in a mouse model of multiple system atrophy (MSA).³

1.Wagner, J., Ryazanov, S., Leonov, A., et al.Anle138b: A novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's diseaseActa Neuropathol.125(6)795-813(2013) 2.Brendel, M., Deussing, M., Blume, T., et al.Late-stage Anle138b treatment ameliorates tau pathology and metabolic decline in a mouse model of human Alzheimer's disease tauAlzheimers Res. Ther.11(1)67(2019) 3.Heras-Garvin, A., Weckbecker, D., Ryazanov, S., et al.Anle138b modulates α-synuclein oligomerization and prevents motor decline and neurodegeneration in a mouse model of multiple system atrophyMov. Disord.34(2)255-263(2019)

Protocol

Kinase experiment:

Compounds (Anle138b) are diluted into the assay mixture from 10-fold stock solutions containing 10 % DMSO (v/v), resulting in a final concentration of 1 % DMSO in all samples. Experiments are started by diluting the 5-fold stock solution of fluorescently labelled α-syn in 50 mM Tris-buffer, pH 7.0, containing 1 % DMSO, 10 μM FeCl3 and compounds (Anle138b) in concentrations ranging from 1-10 μM. Aggregation is monitored at room temperature for at least 2.5 h in 3-4 independent samples for each experimental group[1].

Animal experiment:

Mice: During the first 2 weeks of treatment, 2 mg of anle138b dissolved in 10 μL DMSO mixed with 200 μL peanut butter are given. After 2 weeks of treatment, the dose is increased to 5 mg in 10 μL DMSO/200 μL peanut butter. At the age of 33 weeks, the dose is increased to 2×5 mg per day. All mice are monitored daily for signs of disease[1].

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]. Wagner J, et al. Reducing tau aggregates with anle138b delays disease progression in a mouse model of tauopathies. Acta Neuropathol. 2015 Nov;130(5):619-31.