1201323-97-8

1201323-97-8 structure
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
  • 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
Synonyms MK-3328
Description MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
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

[1]. Harrison ST, et al. Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as β-Amyloid PET Ligands and Identification of MK-3328. ACS Med Chem Lett. 2011 Apr 18;2(7):498-502.

Molecular Formula C14H9FN4O
Molecular Weight 268.24600
Exact Mass 268.07600
PSA 56.74000
LogP 2.91560
Storage condition 2-8℃