1201323-97-8
1201323-97-8 structure
- Name: MK-3328
- Chemical Name: 5-fluoro-2-(1-methylpyrrolo[2,3-b]pyridin-5-yl)-[1,3]oxazolo[5,4-b]pyridine
- CAS Number: 1201323-97-8
- Molecular Formula: C14H9FN4O
- Molecular Weight: 268.24600
- Catalog: Signaling Pathways Neuronal Signaling Amyloid-β
- Create Date: 2017-08-02 22:54:30
- Modify Date: 2024-01-09 18:46:01
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MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
| Name | 5-fluoro-2-(1-methylpyrrolo[2,3-b]pyridin-5-yl)-[1,3]oxazolo[5,4-b]pyridine |
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| Synonyms | MK-3328 |
| Description | MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM. |
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| Related Catalog | |
| Target |
IC50: 10.5 nM (β-Amyloid)[1] |
| In Vitro | MK-3328 exhibits amyloid binding potency balanced with low levels of nonspecific binding[1]. |
| In Vivo | In vivo, [18F]MK-3328 demonstrates favorable kinetics, exhibiting high brain uptake and good washout in normal rhesus monkey positron emission tomography (PET) imaging studies[1]. |
| Kinase Assay | [3H]-DMAB is synthesized at a specific activity of ~80 Ci/mmol. The final concentration of radioligand for tissue homogenate binding assay is 1.5nM. Brain homogenates are diluted with PBS to 0.4 mg/mL from original 10 mg/mL volume and 200 μL is used in assay for a final concentration of 50 μg/assay tube. Unlabeled test compounds are dissolved in DMSO at 1 mM. Dilution of test compound (e.g., MK-3328) to various concentrations is made with PBS containing 2% DMSO. Total binding is defined in the absence of competing compound, and non-displaceable binding is determined in the presence of 1 μM unlabeled self block. Compound dilutions (10×) are added into the assay tube (25 μL each/per tube, separately) containing 200 μL brain homogenate dilution, and the tubes are pre-incubated at room temperature for 10 minutes. Then radioligand dilutions (10×) are added into the assay tube (25 μL each/per tube, separately) to a final volume of 250 μL per tube. Incubation is carried out at room temperature (25°C) for 90 minutes, and then the assay samples are filtered onto GF/C filters using Skatron 12 well harvester, washing on setting 5-5-5 (~ 3×2 mL) ice cold buffer (PBS, pH 7.4). GF/C filter papers for the Skatron harvester are pre-soaked in 0.1% BSA for 1 hour at room temperature before use. Filters are punched into scintillation vials and counted in 2 mL Ultima Gold on Perkin Elmer Tri-Carb 2900TR for 1 minute. The data analysis is done with Prism software. All assays are done in triplicate, and in the laboratory designated for studies using human tissues[1]. |
| References |
| Molecular Formula | C14H9FN4O |
|---|---|
| Molecular Weight | 268.24600 |
| Exact Mass | 268.07600 |
| PSA | 56.74000 |
| LogP | 2.91560 |
| Storage condition | 2-8℃ |