| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
MK-8719 targets O-GlcNAcase (OGA), an enzyme that removes O-GlcNAc modifications from proteins. By inhibiting OGA, MK-8719 increases the levels of O-GlcNAcylated proteins, which is implicated in the regulation of various cellular processes, including those relevant to neurodegenerative diseases such as Alzheimer's disease and tauopathies.
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|---|---|
| ln Vitro |
In vitro, MK-8719 potently inhibits human O-GlcNAcase (hOGA) with a Ki of 7.9 nM. It is highly selective for OGA over other enzymes. The compound shows good CNS penetration, making it suitable for studying OGA function in the brain. Specific cellular activity data are not detailed in the available sources.
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| ln Vivo |
MK-8719 exhibits good intrinsic effectiveness and selectivity, enhanced Papp, high CNS exposure, decent pharmacokinetics, good stability and significant pharmacodynamic response [1].
In vivo activity data for MK-8719 are not extensively detailed in the available sources. The compound is noted to have good central nervous system (CNS) penetration, suggesting it can reach brain targets. It is being developed for potential therapeutic applications in CNS disorders, though specific in vivo efficacy data are not provided. |
| Enzyme Assay |
The in vitro enzyme assay for MK-8719 involves measuring the inhibition of O-GlcNAcase (OGA) activity. Recombinant human OGA is incubated with a fluorogenic substrate (e.g., 4-methylumbelliferyl N-acetyl-β-D-glucosaminide) in the presence of varying compound concentrations. The Ki value is determined by quantifying the reduction in substrate hydrolysis.
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| Cell Assay |
Cellular assays for MK-8719 are not specifically described in the available sources. As an OGA inhibitor, it is typically evaluated in cell-based systems by measuring the increase in O-GlcNAc levels on proteins using Western blotting with O-GlcNAc-specific antibodies. CNS penetration is assessed in cell-based models or in vivo.
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| Animal Protocol |
In vivo animal studies for MK-8719 are not detailed in the available sources. The compound is noted to have good central nervous system (CNS) penetration, which is likely evaluated in rodent models by measuring brain concentrations after administration. Specific animal models and dosing regimens are not described.
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| ADME/Pharmacokinetics |
MK-8719 has good central nervous system (CNS) penetration, indicating favorable pharmacokinetic properties for brain targeting. The compound is a small molecule with a molecular weight of 268.28 g/mol. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for MK-8719 are not reported in the available sources. As an investigational compound, it is used for research purposes only. The compound has been evaluated in preclinical studies, but specific toxicological profiles are not available.
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| References | |
| Additional Infomation |
MK-8719 is a research compound being investigated for potential therapeutic applications in neurodegenerative diseases, particularly those involving O-GlcNAc dysregulation. It is a potent and selective OGA inhibitor with good CNS penetration. The compound is available from chemical suppliers for research use only.
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| Molecular Formula |
C9H14F2N2O3S
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|---|---|
| Molecular Weight |
268.2809
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| Exact Mass |
268.07
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| Elemental Analysis |
C, 40.29; H, 5.26; F, 14.16; N, 10.44; O, 17.89; S, 11.95
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| CAS # |
1382799-40-7
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| PubChem CID |
136416849
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
319
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| Defined Atom Stereocenter Count |
5
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| Synonyms |
MK-8719; MK 8719; MK8719;
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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 |
| 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 : ~100 mg/mL (~372.74 mM)
H2O : ≥ 6.67 mg/mL (~24.86 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.32 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 (9.32 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7274 mL | 18.6372 mL | 37.2745 mL | |
| 5 mM | 0.7455 mL | 3.7274 mL | 7.4549 mL | |
| 10 mM | 0.3727 mL | 1.8637 mL | 3.7274 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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