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| Targets |
PBB3 targets tau protein aggregates in the brain. Tau is a microtubule-associated protein that, in pathological conditions, forms neurofibrillary tangles and other aggregates. These aggregates are a hallmark of Alzheimer's disease and other tauopathies. PBB3 is a selective PET ligand that binds to tau pathology in the brain. By binding to tau aggregates, PBB3 enables the visualization and quantification of tau pathology using PET imaging. This allows researchers to study the progression of tau pathology in neurodegenerative diseases.
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| ln Vitro |
In vitro, PBB3 has been shown to bind to tau aggregates in brain tissue from Alzheimer's disease patients. It can be used to detect tau pathology in post-mortem brain sections. PBB3 (56.5 μM) has been used to fluorescently label brain pathological changes in Alzheimer's disease patients. The compound's selectivity for tau over amyloid-β has been confirmed in binding studies. These in vitro studies validate PBB3 as a specific tau PET tracer.
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| ln Vivo |
In vivo, PBB3 is used as a PET tracer to image tau pathology in the living human brain. It can be used to detect tau pathology in Alzheimer's disease and non-Alzheimer's disease tauopathies. PBB3 can more clearly detect dystrophic neurites and diffuse neurofibrillary tangles with calcification in the Alzheimer's disease brain. The tracer enables the longitudinal monitoring of tau pathology progression and the evaluation of potential tau-targeting therapies in clinical trials.
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| Enzyme Assay |
In vitro receptor binding assays for PBB3 measure its affinity for tau protein aggregates. Brain homogenates from Alzheimer's disease patients or recombinant tau aggregates are incubated with radiolabeled PBB3 in the presence of varying concentrations of unlabeled PBB3. The Ki is determined from competition binding curves. Selectivity is assessed by testing the compound against amyloid-β aggregates and other proteins. These assays confirm PBB3's specificity for tau pathology.
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| Cell Assay |
In vitro cell-based assays for PBB3 are not typically performed, as the compound is a PET tracer used for imaging. However, its binding to tau aggregates can be studied using tau-overexpressing cell lines or primary neurons. Cells are treated with PBB3, and the binding is assessed by fluorescence microscopy or flow cytometry. These assays confirm the compound's cellular binding to tau aggregates.
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| Animal Protocol |
In vivo animal experiments for PBB3 are conducted in animal models of tauopathy. In a typical study, PBB3 is administered to transgenic mice expressing human tau or to mice injected with tau aggregates. The tracer's biodistribution and binding to tau pathology in the brain are assessed using PET imaging or autoradiography. These studies validate PBB3 as a tau PET tracer and provide data on its pharmacokinetics and specificity in vivo.
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| ADME/Pharmacokinetics |
PBB3 has a molecular weight of 309.39 g/mol and a molecular formula of C17H15N3OS. It is a solid compound. For storage, it is recommended to keep the powder at -20°C for up to 3 years. In solvent, it can be stored at -80°C for 1 year. The compound is shipped with blue ice or at ambient temperature. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized in the context of PET imaging studies.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PBB3 is not provided in standard product descriptions. As a PET tracer, it is administered in very small amounts (microdoses) for imaging purposes, and its toxicity is expected to be minimal. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling PBB3. Its use is limited to research applications.
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| References | |
| Additional Infomation |
PBB3 is a research compound and is not approved for any clinical or therapeutic use. It is a tau-specific PET tracer used to detect and quantify tau protein aggregates in the brain. PBB3 can be used to detect tau pathology in Alzheimer's disease and non-Alzheimer's disease tauopathies. It is a valuable research tool for studying the progression of tau pathology in neurodegenerative diseases and for evaluating potential tau-targeting therapies. PBB3 is not a therapeutic agent.
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| Exact Mass |
309.093
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|---|---|
| CAS # |
1565796-97-5
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| PubChem CID |
73330716
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
572.4±60.0 °C at 760 mmHg
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| Flash Point |
300.0±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.797
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
415
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(/C=C/C=C/C2=CN=C(C=C2)NC)=NC2C=CC(=CC1=2)O
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| InChi Key |
LBCRWMJTAFCLCL-ZUVMSYQZSA-N
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| InChi Code |
InChI=1S/C17H15N3OS/c1-18-16-9-6-12(11-19-16)4-2-3-5-17-20-14-8-7-13(21)10-15(14)22-17/h2-11,21H,1H3,(H,18,19)/b4-2+,5-3+
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| Chemical Name |
2-[(1E,3E)-4-[6-(methylamino)pyridin-3-yl]buta-1,3-dienyl]-1,3-benzothiazol-6-ol
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| Synonyms |
PBB3 PBB-3 J3.303.052E
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06344845 | RECRUITING | Diagnostic Test: 18F-PBB3 PET/CT scan | Neurodegenerative Diseases | Peking Union Medical College Hospital | 2022-11-01 | Not Applicable |
| NCT04305210 | UNKNOWN STATUS | Drug: F-18 PMPBB3 Drug: 18F-florbetapir |
Alzheimer's Disease | Chang Gung Memorial Hospital | 2019-12-01 | Phase 2 |
| NCT04248270 | UNKNOWN STATUS | Drug: 18F-PM-PBB3 | Alzheimer's Disease Dementia Vascular Dementia |
Chang Gung Memorial Hospital | 2020-02-20 | Phase 1 Phase 2 |
| NCT03625128 | COMPLETED | Drug: F-18 | Alzheimer's Disease Cortical Basal Syndrome Frontotemporal Dementia Progressive Supranuclear Palsy Vascular Cognitive Impairment |
Chang Gung Memorial Hospital | 2018-01-02 | Early Phase 1 |
| NCT05003830 | RECRUITING | Device: PET/MR | Alzheimer Disease PET/MR |
Wuhan Union Hospital, China | 2020-07-01 |
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