TB5
目录号 : GC30988
A potent and selective MAO-B inhibitor
Cas No.:948841-07-4
Sample solution is provided at 25 µL, 10mM.
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TB5 is a potent and selective monoamine oxidase B (MAO-B) inhibitor with Ki values of 110 and 1,450 nM for MAO-B and MAO-A, respectively.1 It interacts with the catalytic site of human MAO-B in a competitive manner. In an enzyme assay, MAO-B activity increases?from 37% to 97% following inhibitor washout, indicating TB5 binding is reversible.?TB5 also demonstrates permeability in a parallel artificial membrane permeation assay (PAMPA), a model for the blood-brain barrier, and has minimal cytotoxicity (>84% cell viability) in HepG2 cells at a concentrations up to 25 μM.
1.Mathew, B., Haridas, A., U?ar, G., et al.Synthesis, biochemistry, and computational studies of brominated thienyl chalcones: A new class of reversible MAO-B inhibitorsChemMedChem11(11)1161-1171(2016)
Kinase experiment: | Compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The set consists of five graphs, each constructed by measuring MAO-B and MAO-A catalytic rates at different substrate concentrations (0.1-1 μM). The first Lineweaver–Burk plot is constructed in the absence of inhibitor, while the remaining four graphs are constructed in the presence of different concentrations of TB5 and TB8[1]. |
Cell experiment: | In vitro cytotoxicity of brominated thiophene chalcones and standard MAO inhibitors are tested in human HepG2 hepatic cancer cells at three different concentrations (1, 5 and 25 μM)[1]. |
References: [1]. Mathew B, et al. Synthesis, Biochemistry, and Computational Studies of Brominated Thienyl Chalcones: A New Class of Reversible MAO-B Inhibitors. ChemMedChem. 2016 Jun 6;11(11):1161-71. | |
| Cas No. | 948841-07-4 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(Br)S1)/C=C/C2=CC=C(N(C)C)C=C2 | ||
| 分子式 | C15H14BrNOS | 分子量 | 336.25 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 1 mg/ml | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.974 mL | 14.8699 mL | 29.7398 mL |
| 5 mM | 0.5948 mL | 2.974 mL | 5.948 mL |
| 10 mM | 0.2974 mL | 1.487 mL | 2.974 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