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PBT 1033

(Synonyms: PBT 2) 目录号 : GC67707

PBT 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。

PBT 1033 Chemical Structure

Cas No.:747408-78-2

规格 价格 库存 购买数量
10mg
¥1,980.00
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25mg
¥4,050.00
现货
50mg
¥6,480.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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.

Chemical Properties

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
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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
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