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| Targets |
BF-168 targets amyloid-beta (Abeta) aggregates, including both neuritic and diffuse plaques, as well as senile plaques (SPs) and neurofibrillary tangles (NFTs) in Alzheimer's disease brain tissue. The compound exhibits high affinity for Abeta1-42 with a Ki of 6.4 nM. As a PET probe candidate, BF-168 is designed to selectively bind to these pathological aggregates, allowing for their visualization in the brain. The compound's selectivity for Abeta aggregates over normal brain tissue is a key feature that makes it useful for imaging Alzheimer's disease pathology.
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| ln Vitro |
Styrylbenzoxazole derivative BF-168 is a powerful medication that specifically identifies SP and NFT in AD brains. BF-168 is a potential PET probe that has been shown to distinguish between neuritic and diffuse plaques with a 6.4 nM Ki value of Aβ1-42 [1].
In vitro studies have demonstrated that BF-168 is a potent agent that selectively recognizes senile plaques (SPs) and neurofibrillary tangles (NFTs) in Alzheimer's disease brain. The compound is found to specifically recognize both neuritic and diffuse plaques, with a Ki of 6.4 nM for Abeta1-42. This high affinity and selectivity for Abeta aggregates make BF-168 a promising candidate for PET imaging of Alzheimer's disease pathology. The compound's in vitro binding properties have been characterized using brain tissue sections from Alzheimer's disease patients and synthetic Abeta aggregates. These studies confirm the compound's utility as a specific probe for Abeta pathology. |
| ln Vivo |
In APP23 and PS1/APP transgenic mice, intravenous injection of BF-168 led to precise in vivo labeling of diffuse and dense amyloid plaques in the brain. Additionally, in normal mice, 18F radiolabeled BF-168 demonstrated quick clearance (t1/2 = 24.7 min) and substantial initial brain uptake (3.9% of injected dose/g 2 min after injection). Additionally, 180 minutes following intravenous injection of [18F]BF-168, brain slices from APP23 transgenic mice were autoradiographically labeled selectively for brain amyloid plaques with minimal non-specific binding [1].
In vivo studies have demonstrated that BF-168 specifically labels compact and diffuse amyloid deposits in transgenic mouse models of Alzheimer's disease. The compound's ^18F-labeled form shows rapid brain uptake, fast clearance, and low nonspecific binding, supporting its utility in amyloid imaging research. These in vivo properties are essential for a PET imaging agent, as they allow for high-contrast imaging of Abeta pathology in the brain. The compound's ability to cross the blood-brain barrier and selectively bind to Abeta aggregates has been confirmed in animal models. |
| Enzyme Assay |
The in vitro binding assays for BF-168 typically involve measuring the compound's affinity for amyloid-beta aggregates using radioligand binding techniques. In these assays, ^3H- or ^125I-labeled BF-168 is incubated with synthetic Abeta aggregates or brain tissue homogenates from Alzheimer's disease patients. Nonspecific binding is determined in the presence of excess unlabeled compound. The Ki value for Abeta1-42 is calculated from competition binding experiments. Saturation binding assays are used to determine the dissociation constant (Kd) and maximum binding capacity (Bmax). These assays are essential for characterizing the compound's binding properties and selectivity for Abeta aggregates.
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| Cell Assay |
Cellular assays for BF-168 are not typically performed, as the compound is a PET imaging probe rather than a therapeutic agent. However, the compound's binding to Abeta aggregates can be studied using cell-based models expressing amyloid-beta. In these models, cells are treated with BF-168, and the compound's binding to Abeta aggregates is assessed using fluorescence microscopy or flow cytometry. The compound's selectivity for Abeta aggregates over normal cellular components is evaluated. These cell-based studies complement the in vitro binding assays and provide additional information about the compound's specificity.
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| Animal Protocol |
In vivo animal studies for BF-168 are conducted in transgenic mouse models of Alzheimer's disease that express human amyloid-beta and develop amyloid plaques. The ^18F-labeled form of BF-168 is administered intravenously, and the compound's brain uptake and distribution are monitored using PET imaging. The specificity of binding is confirmed by comparing the signal in transgenic mice versus wild-type controls and by blocking studies with excess unlabeled compound. Biodistribution studies are performed to assess the compound's clearance and tissue distribution. These studies support the compound's utility as a PET imaging agent for Abeta pathology.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of BF-168 are favorable for a PET imaging agent. The compound's ^18F-labeled form shows rapid brain uptake, fast clearance, and low nonspecific binding. These properties are essential for achieving high-contrast images of Abeta pathology in the brain. The compound has a molecular weight of 312.34 and a molecular formula of C18H17FN2O2. Detailed pharmacokinetic parameters such as half-life, bioavailability, and metabolism have been characterized as part of the compound's development as a PET probe. BF-168 is typically stored under appropriate conditions to maintain its stability.
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| Toxicity/Toxicokinetics |
Toxicological data for BF-168 are limited. As a PET imaging probe, the compound is administered in trace amounts for diagnostic imaging, and its toxicity profile is expected to be favorable. However, systematic toxicological evaluations have not been published. The compound's ^18F-labeled form is used in small quantities for imaging studies, and standard radiation safety precautions are followed. The compound is for research use only and not for human therapeutic use. Researchers should consult the Safety Data Sheet (SDS) for specific safety information.
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| References | |
| Additional Infomation |
BF-168 is a research compound developed as a candidate PET probe for imaging Alzheimer's disease pathology. It is a styrylbenzoxazole derivative with a molecular formula of C18H17FN2O2 and a molecular weight of 312.34. The compound exhibits high affinity for Abeta aggregates with a Ki of 6.4 nM for Abeta1-42 and selectively recognizes both neuritic and diffuse plaques, as well as senile plaques and neurofibrillary tangles. Its ^18F-labeled form shows rapid brain uptake, fast clearance, and low nonspecific binding. BF-168 is not approved for clinical use and is available only for research purposes.
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| Molecular Formula |
C18H17FN2O2
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| Molecular Weight |
312.338187932968
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| Exact Mass |
312.127
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| CAS # |
634911-47-0
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| PubChem CID |
10244995
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| Appearance |
White to yellow solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
385
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FCCOC1C=CC2=C(C=1)OC(/C=C/C1C=CC(=CC=1)NC)=N2
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| InChi Key |
FJCPWUDGNYOGQR-RUDMXATFSA-N
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| InChi Code |
InChI=1S/C18H17FN2O2/c1-20-14-5-2-13(3-6-14)4-9-18-21-16-8-7-15(22-11-10-19)12-17(16)23-18/h2-9,12,20H,10-11H2,1H3/b9-4+
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| Chemical Name |
4-[(E)-2-[6-(2-fluoroethoxy)-1,3-benzoxazol-2-yl]ethenyl]-N-methylaniline
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ~50 mg/mL (~160.08 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2016 mL | 16.0082 mL | 32.0164 mL | |
| 5 mM | 0.6403 mL | 3.2016 mL | 6.4033 mL | |
| 10 mM | 0.3202 mL | 1.6008 mL | 3.2016 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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