| Size | Price | Stock | Qty |
|---|---|---|---|
| 25g |
|
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| Other Sizes |
| Targets |
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone targets monoamine oxidase A (MAO-A) with an IC50 of 0.87 μM and Ki of 0.32 μM [1]
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone targets monoamine oxidase B (MAO-B) with an IC50 of 2.6 μM and Ki of 0.95 μM [1] |
|---|---|
| ln Vitro |
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone has no effect on MAO-B and has an IC50 of 183 μM, making it a weak inhibitor of MAO-A [1].
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone (0.1 μM–10 μM) dose-dependently inhibited MAO-A and MAO-B activities. For MAO-A, maximal inhibition (>90%) was achieved at 10 μM; for MAO-B, maximal inhibition (82%) was achieved at 10 μM [1] Lineweaver-Burk kinetic analysis revealed that the compound acts as a competitive inhibitor of both MAO-A and MAO-B, with increased Km values and unchanged Vmax, indicating binding to the active site of the enzymes [1] The compound showed higher selectivity for MAO-A over MAO-B, with a selectivity index (MAO-B IC50 / MAO-A IC50) of 3.0 [1] |
| Enzyme Assay |
MAO-A inhibition assay: Recombinant human MAO-A enzyme was incubated with different concentrations of 7-Hydroxy-3,4-dihydro-2(1H)-quinolinone (0.1 μM–10 μM) in assay buffer at 37°C for 15 minutes. 5-Hydroxytryptamine was added as the specific substrate to initiate the reaction, and the mixture was incubated for another 30 minutes. The reaction product was detected by a fluorometric method, and the inhibition rate was calculated. IC50 values were obtained by fitting dose-response curves, and Ki values were determined using the Cheng-Prusoff equation [1]
MAO-B inhibition assay: Recombinant human MAO-B enzyme was used, with benzylamine as the specific substrate. The assay protocol was identical to that for MAO-A, including incubation conditions, substrate addition, and product detection. IC50 and Ki values were calculated using the same methods [1] Kinetic analysis assay: For both MAO-A and MAO-B, the enzyme was incubated with 7-Hydroxy-3,4-dihydro-2(1H)-quinolinone at fixed concentrations (0, 0.5, 1, 2 μM for MAO-A; 0, 1, 2, 4 μM for MAO-B) and varying substrate concentrations. Initial reaction rates were measured, and Lineweaver-Burk plots were generated to determine the inhibition type [1] |
| References | |
| Additional Infomation |
7-Hydroxy-3,4-dihydrocarboxylon belongs to the quinoline class of compounds. 7-Hydroxy-3,4-dihydro-2(1H)-quinolinelonone is a synthetic derivative of 3,4-dihydro-2(1H)-quinolinelonone, which is a skeleton with potential monoamine oxidase inhibitory activity [1]. The monoamine oxidase inhibitory activity of this compound suggests its potential application in the treatment of neuropsychiatric disorders (e.g., depression, anxiety) and neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's disease) involving monoamine neurotransmitter dysregulation [1]. The competitive inhibition mechanism indicates that this compound interacts with the substrate-binding pocket of monoamine oxidase, a common mechanism of action for clinically used monoamine oxidase inhibitors [1].
|
| Molecular Formula |
C9H9NO2
|
|---|---|
| Molecular Weight |
163.17326
|
| Exact Mass |
163.063
|
| CAS # |
22246-18-0
|
| PubChem CID |
2785758
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
403.7±45.0 °C at 760 mmHg
|
| Melting Point |
233-237 °C
|
| Flash Point |
198.0±28.7 °C
|
| Vapour Pressure |
0.0±1.0 mmHg at 25°C
|
| Index of Refraction |
1.604
|
| LogP |
0.99
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
12
|
| Complexity |
193
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LKLSFDWYIBUGNT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H9NO2/c11-7-3-1-6-2-4-9(12)10-8(6)5-7/h1,3,5,11H,2,4H2,(H,10,12)
|
| Chemical Name |
7-hydroxy-3,4-dihydro-1H-quinolin-2-one
|
| 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 (~612.86 mM)
H2O : ~1 mg/mL (~6.13 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.32 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 (15.32 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 (15.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1 mg/mL (6.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1286 mL | 30.6429 mL | 61.2858 mL | |
| 5 mM | 1.2257 mL | 6.1286 mL | 12.2572 mL | |
| 10 mM | 0.6129 mL | 3.0643 mL | 6.1286 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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