| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Copper and zinc ionophore; also modulates metal ion homeostasis in the brain. PBT 1033 facilitates the transport of copper and zinc ions across cellular membranes, thereby restoring metal ion balance in neurodegenerative conditions. It induces the uptake of zinc, copper, and iron in M17 neuroblastoma cells at concentrations of 2-10 µM.
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| ln Vitro |
PB 1033 exhibits antimicrobial activity directed against S. uberis, possessing a 14.5 μM MIC value [2]. NEUROSCITOtoxicity caused by glutamate is prevented by PBT2 (1, 3 and 7.5 μM, 6 h)[3]. NMDAR-mediated Ca2+ flux in mouse cortical neurons is decreased by PBT2 (10 μM, 1 or 6 h)[3]. In SH-SY5Y cells, GSK3α/β phosphorylation is increased by PBT2 (0-10 μM, 1 h)[4]. Zn-induced protease-resistant Aβ aggregates are inhibited from forming by PBT2 (20 μM, 1 h)[5].
In vitro, PBT 1033 induces the uptake of zinc, copper, and iron in M17 neuroblastoma cells when used at concentrations ranging from 2 to 10 µM. It shows antimicrobial properties against Gram-positive bacteria. The compound's ionophore activity promotes metal ion redistribution, which is believed to contribute to its neuroprotective effects by reducing metal-induced oxidative stress and protein aggregation. |
| ln Vivo |
In a mouse model of Alzheimer's disease, PBT 1033 (30 mg/kg/d, po, 11 days) restores the biochemical substrates of learning and memory[5].
In vivo, PBT 1033 restores cognitive abilities in mouse models of Alzheimer's disease. Oral administration of the compound improves cognitive function and reduces amyloid-beta pathology in transgenic AD mouse models. It also shows potential neuroprotective effects in models of Huntington's disease, making it a promising candidate for neurodegenerative disease research. |
| Enzyme Assay |
Ionophore activity is assessed by measuring metal ion uptake in cultured cells using fluorescent metal indicators (e.g., FluoZin-3 for zinc, Phen Green SK for copper) or atomic absorption spectroscopy. Cells are treated with PBT 1033 (2-10 µM) and metal ion concentrations are quantified. Antimicrobial activity is evaluated using standard broth microdilution assays against Gram-positive bacterial strains to determine minimum inhibitory concentrations (MICs).
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| Cell Assay |
Western Blot Analysis[4]
Cell Types: SH-SY5Y cells Tested Concentrations: 0-10 μM Incubation Duration: 1 h Experimental Results: Increased in cellular levels of GSK3α/β phosphorylated at the inhibitory serine 21/9 residue (ser21/9 on GSK3α/β). M17 neuroblastoma cells are cultured in appropriate medium and treated with PBT 1033 at concentrations ranging from 2 to 10 µM for specified time periods. Cellular metal content (zinc, copper, iron) is measured using inductively coupled plasma mass spectrometry (ICP-MS) or fluorescent probes. Cell viability is assessed to confirm that observed effects are not due to cytotoxicity. |
| Animal Protocol |
Animal/Disease Models: Female Tg2576 mice[5]
Doses: 30 mg/kg/d Route of Administration: Oral administration, 11 days Experimental Results: Increased hippocampal apical spine density, basal spine density. Alzheimer's disease transgenic mouse models (e.g., APP/PS1 or Tg2576) are treated with PBT 1033 via oral gavage at doses determined from pharmacokinetic studies. Cognitive function is assessed using Morris water maze, novel object recognition, or Y-maze tests. Brain tissue is harvested for amyloid-beta quantification, metal ion analysis, and histopathological examination of plaque burden and neuronal health. |
| ADME/Pharmacokinetics |
PBT 1033 is an orally bioavailable compound with molecular formula C12H12Cl2N2O and molecular weight 271.14. It shows good solubility in DMSO (100 mg/mL, 368.80 mM). The compound is formulated for oral administration and demonstrates favorable absorption characteristics. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability require further characterization from published studies.
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| Toxicity/Toxicokinetics |
No significant toxicity has been reported in preclinical studies at therapeutic doses. The compound shows a favorable safety profile in animal models. Standard toxicological evaluations, including acute and subchronic toxicity studies, would be required for full safety characterization. The compound is generally well-tolerated at doses that produce cognitive improvement in mouse models.
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| References |
[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. |
| Additional Infomation |
Drug Indication
It has been studied for the treatment of Alzheimer's disease. PBT 1033 (also known as PBT 2, PB 1033) is a potential neuroprotective agent for Alzheimer's disease and Huntington's disease research. It is a copper/zinc ionophore with molecular formula C12H12Cl2N2O and CAS number 747408-78-2. The compound is supplied as a light yellow to brown solid powder with purity ≥98%. It has not received FDA approval and is for research use only. Synonyms include PBT-2, PBT2, and PBT1033. |
| Molecular Formula |
C12H12CL2N2O
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| Molecular Weight |
271.14
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| Exact Mass |
270.032
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| CAS # |
747408-78-2
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| PubChem CID |
10016012
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
367.8±37.0 °C at 760 mmHg
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| Flash Point |
176.2±26.5 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.654
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| LogP |
3.51
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
265
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(Cl)=C(C2=C(C=CC(CN(C)C)=N2)C=1Cl)O
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| InChi Key |
YZPOQCQXOSEMAZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12Cl2N2O/c1-16(2)6-7-3-4-8-9(13)5-10(14)12(17)11(8)15-7/h3-5,17H,6H2,1-2H3
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| Chemical Name |
5,7-dichloro-2-[(dimethylamino)methyl]quinolin-8-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (368.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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