| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg | |||
| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Flobetapir targets β-amyloid (Aβ) plaques, which are a hallmark of Alzheimer's disease pathology. The compound is a fluoropegylated stilbene derivative with a styrylpyridine nucleus that binds to β-amyloid plaques. When labeled with fluorine-18, flobetapir serves as a PET tracer that allows for the non-invasive visualization of Aβ plaque burden in the living brain.
|
|---|---|
| ln Vitro |
One potentially well-tolerated imaging agent is flobetapir [1].
Flobetapir binds to β-amyloid plaques with high affinity and specificity. The compound's binding to Aβ aggregates can be assessed in vitro using brain tissue sections from Alzheimer's disease patients or using synthetic Aβ fibrils. In vitro binding assays measure the displacement of a radiolabeled Aβ ligand (e.g., [³H]-PIB) by flobetapir to determine its affinity for Aβ aggregates. |
| ln Vivo |
Flobetapir is used in vivo as a PET imaging agent for the detection of β-amyloid plaques in the brain. It is administered intravenously to patients, and PET scans are performed to visualize the distribution of the tracer in the brain. The compound is used clinically to assist in the diagnosis of Alzheimer's disease and in research to monitor disease progression and evaluate therapeutic efficacy.
|
| Enzyme Assay |
For non-cellular assays, flobetapir's affinity for β-amyloid aggregates can be evaluated using in vitro binding studies. Synthetic Aβ1-42 fibrils or Alzheimer's disease brain homogenates are incubated with [¹⁸F]-flobetapir or a related radiolabeled compound and varying concentrations of unlabeled flobetapir. Binding displacement curves are generated to determine the IC₅₀ and Ki values for binding to Aβ aggregates.
|
| Cell Assay |
In vitro cellular assays for flobetapir are limited as the compound is a PET imaging agent rather than a therapeutic compound. Its binding to Aβ aggregates can be assessed in cell-based models that express or accumulate Aβ, but these are not standard assays for this compound. The compound's primary application is in vivo imaging.
|
| Animal Protocol |
In vivo animal experiments with flobetapir involve administering the radiolabeled compound to transgenic mouse models of Alzheimer's disease (e.g., APP/PS1 mice) that develop Aβ plaques. PET imaging is performed to visualize the tracer's distribution in the brain. The compound's ability to detect Aβ plaques is validated by comparing PET signals with post-mortem histological analysis of brain tissue.
|
| ADME/Pharmacokinetics |
Flobetapir has a molecular weight of 360.42 and a molecular formula of C₂₀H₂₅FN₂O₃. The radiolabeled form, florbetapir F 18, contains the radionuclide fluorine-18. The compound is supplied as an injectable solution for intravenous administration. It is typically stored at controlled room temperature and protected from radiation. The half-life of ¹⁸F is approximately 110 minutes, requiring timely administration after synthesis.
|
| Toxicity/Toxicokinetics |
Flobetapir is generally well-tolerated as a diagnostic imaging agent. Adverse reactions are rare but can include headache, nausea, and injection site reactions. As with all radiopharmaceuticals, there is a small radiation exposure risk. The compound should be used with caution in patients with renal impairment.
|
| References | |
| Additional Infomation |
Flobetapir (AV-45) is a PET imaging agent used for the detection of β-amyloid plaques in the brain. It is used clinically to assist in the diagnosis of Alzheimer's disease and in research to monitor disease progression. The compound is a fluoropegylated stilbene derivative that binds to Aβ plaques. It is available as florbetapir F 18 for clinical and research use.
|
| Molecular Formula |
C20H25FN2O3
|
|---|---|
| Molecular Weight |
360.422508955002
|
| Exact Mass |
360.184
|
| CAS # |
938435-69-9
|
| PubChem CID |
57396865
|
| Appearance |
Light brown to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
524.7±50.0 °C at 760 mmHg
|
| Flash Point |
271.1±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.592
|
| LogP |
3.07
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
26
|
| Complexity |
376
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FCCOCCOCCOC1C=CC(=CN=1)/C=C/C1C=CC(=CC=1)NC
|
| InChi Key |
YNDIAUKFXKEXSV-NSCUHMNNSA-N
|
| InChi Code |
InChI=1S/C20H25FN2O3/c1-22-19-7-4-17(5-8-19)2-3-18-6-9-20(23-16-18)26-15-14-25-13-12-24-11-10-21/h2-9,16,22H,10-15H2,1H3/b3-2+
|
| Chemical Name |
4-[(E)-2-[6-[2-[2-(2-fluoroethoxy)ethoxy]ethoxy]pyridin-3-yl]ethenyl]-N-methylaniline
|
| Synonyms |
AV45 AV 45 AV-45 Flobetapir
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~277.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.94 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 | 2.7745 mL | 13.8727 mL | 27.7454 mL | |
| 5 mM | 0.5549 mL | 2.7745 mL | 5.5491 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7745 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA