PBT 1033
(Synonyms: PBT 2) 目录号 : GC67707PBT 1033 (PBT 2) 是一种具有口服活性的铜/锌离子载体。PBT 1033 可恢复阿尔茨海默病 (AD) 小鼠模型中小鼠的认知能力。PB 1033 还对革兰氏阳性菌具有抗菌活性。
Cas No.:747408-78-2
Sample solution is provided at 25 µL, 10mM.
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PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria[1][2].
PB 1033 displays antibacterial activity against S. uberis, with a MIC value of 14.5 μM[2].
PBT2 (1, 3 and 7.5 μM, 6 h) protects neurons against glutamate-induced excitotoxicity[3].
PBT2 (10 μM, 1 or 6 h) reduces NMDAR-mediated Ca2+ flux in mouse cortical neurons[3].
PBT2 (0-10 μM, 1 h) increases GSK3α/β phosphorylation in SH-SY5Y cells[4].
PBT2 (20 μM, 1 h) prevents the formation of Zn-induced protease resistant Aβ aggregates[5].
Western Blot Analysis[4]
| Cell Line: | SH-SY5Y cells |
| Concentration: | 0-10 μM |
| Incubation Time: | 1 h |
| Result: | Increased in cellular levels of GSK3α/β phosphorylated at the inhibitory serine 21/9 residue (ser21/9 on GSK3α/β). |
PBT 1033 (30 mg/kg/d, p.o., 11 days) restores biochemical substrates of learning/memory in a mouse model of alzheimer's disease[5].
| Animal Model: | Female Tg2576 mice[5] |
| Dosage: | 30 mg/kg/d |
| Administration: | Oral administration, 11 days |
| Result: | Increased hippocampal apical spine density, basal spine density. |
[1]. Faux NG, et al. PBT2 rapidly improves cognition in Alzheimer's Disease: additional phase II analyses. J Alzheimers Dis. 2010;20(2):509-16.
[2]. Harbison-Price N, et al. Multiple Bactericidal Mechanisms of the Zinc Ionophore PBT2. mSphere. 2020 Mar 18;5(2):e00157-20.
[3]. Johanssen T, et al. PBT2 inhibits glutamate-induced excitotoxicity in neurons through metal-mediated preconditioning. Neurobiol Dis. 2015 Sep;81:176-85.
[4]. Crouch PJ, et al. The Alzheimer's therapeutic PBT2 promotes amyloid-β degradation and GSK3 phosphorylation via a metal chaperone activity. J Neurochem. 2011 Oct;119(1):220-30.
[5]. Adlard PA, et al. Metal ionophore treatment restores dendritic spine density and synaptic protein levels in a mouse model of Alzheimer's disease. PLoS One. 2011 Mar 11;6(3):e17669.
| Cas No. | 747408-78-2 | SDF | Download SDF |
| 别名 | PBT 2 | ||
| 分子式 | C12H12Cl2N2O | 分子量 | 271.14 |
| 溶解度 | DMSO : 100 mg/mL (368.81 mM; Need ultrasonic) | 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 | 3.6881 mL | 18.4407 mL | 36.8813 mL |
| 5 mM | 0.7376 mL | 3.6881 mL | 7.3763 mL |
| 10 mM | 0.3688 mL | 1.8441 mL | 3.6881 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