PBT 1033
Based on 1 publication(s) in Google Scholar
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.
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- Pureza: 99.51%
- No. CAS: 747408-78-2
- Fòrmula: C12H12Cl2N2O
- Peso molecular:271.15
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) PBT 1033
More
Actividad biológica
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:0-10 μM
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Incubation Time:1 h
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Result:Increased in cellular levels of GSK3α/β phosphorylated at the inhibitory serine 21/9 residue (ser21/9 on GSK3α/β).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Tg2576 mice[5]
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Dosage:30 mg/kg/d
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Administration:Oral administration, 11 days
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Result:Increased hippocampal apical spine density, basal spine density.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 747408-78-2
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Appearance Solid
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Peso molecular 271.15
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Fòrmula C12H12Cl2N2O
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Color Light yellow to brown
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SMILES
ClC1=CC(Cl)=C(O)C2=C1C=CC(CN(C)C)=N2
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Synonyms
PBT 2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Parasitol Drugs Drug Resist
In vitro and in vivo anti-piroplasm activity of PBT2 against Theileria annulata and Babesia microti. [Abstract]2026 Apr 22:31:100646. PMID: 42030593
Solvente y solubilidad
DMSO : 100 mg/mL (368.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[3]. Johanssen T, et al. PBT2 inhibits glutamate-induced excitotoxicity in neurons through metal-mediated preconditioning. Neurobiol Dis. 2015 Sep;81:176-85. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6880 mL | 18.4402 mL | 36.8804 mL | 92.2009 mL |
| 5 mM | 0.7376 mL | 3.6880 mL | 7.3761 mL | 18.4402 mL | |
| 10 mM | 0.3688 mL | 1.8440 mL | 3.6880 mL | 9.2201 mL | |
| 15 mM | 0.2459 mL | 1.2293 mL | 2.4587 mL | 6.1467 mL | |
| 20 mM | 0.1844 mL | 0.9220 mL | 1.8440 mL | 4.6100 mL | |
| 25 mM | 0.1475 mL | 0.7376 mL | 1.4752 mL | 3.6880 mL | |
| 30 mM | 0.1229 mL | 0.6147 mL | 1.2293 mL | 3.0734 mL | |
| 40 mM | 0.0922 mL | 0.4610 mL | 0.9220 mL | 2.3050 mL | |
| 50 mM | 0.0738 mL | 0.3688 mL | 0.7376 mL | 1.8440 mL | |
| 60 mM | 0.0615 mL | 0.3073 mL | 0.6147 mL | 1.5367 mL | |
| 80 mM | 0.0461 mL | 0.2305 mL | 0.4610 mL | 1.1525 mL | |
| 100 mM | 0.0369 mL | 0.1844 mL | 0.3688 mL | 0.9220 mL |
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