Anle138b
(Synonyms: 3-(1,3-苯并二恶唑-5-基)-5-(3-溴苯基)-1H-吡唑) 目录号 : GC30846
An inhibitor of protein aggregation
Cas No.:882697-00-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Anle138b is an inhibitor of protein aggregation.1 It inhibits α-synuclein oligomer formation and PrPSc prion propagation by 77 and 84%, respectively, when used at a concentration of 10 ?M. Anle138b (1 mg/animal) inhibits brain accumulation of PrPSc 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)
|
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]. |
|
References: [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. |
|
| Cas No. | 882697-00-9 | SDF | |
| 别名 | 3-(1,3-苯并二恶唑-5-基)-5-(3-溴苯基)-1H-吡唑 | ||
| Canonical SMILES | BrC1=CC(C2=CC(C3=CC=C(OCO4)C4=C3)=NN2)=CC=C1 | ||
| 分子式 | C16H11BrN2O2 | 分子量 | 343.17 |
| 溶解度 | DMSO : ≥ 50 mg/mL (145.70 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.914 mL | 14.57 mL | 29.1401 mL |
| 5 mM | 0.5828 mL | 2.914 mL | 5.828 mL |
| 10 mM | 0.2914 mL | 1.457 mL | 2.914 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet