MK-3328 |
| رقم الكتالوجGC31285 |
MK-3328 عبارة عن يجند β-Amyloid PET ، والذي يُظهر فاعلية ربط عالية مع IC50 يبلغ 10.5 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1201323-97-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
MK-3328 exhibits amyloid binding potency balanced with low levels of nonspecific binding[1].
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].
[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.
Kinase experiment: | [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. | |
| Cas No. | 1201323-97-8 | SDF | |
| Canonical SMILES | CN1C=CC2=CC(C3=NC4=CC=C(F)N=C4O3)=CN=C21 | ||
| Formula | C14H9FN4O | M.Wt | 268.25 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7279 mL | 18.6393 mL | 37.2787 mL |
| 5 mM | 0.7456 mL | 3.7279 mL | 7.4557 mL |
| 10 mM | 0.3728 mL | 1.8639 mL | 3.7279 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *