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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C13H17ClN2O2 |
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分子量 | 268.74 | CAS No. | 71320-77-9 | |
Solubility (25°C)* | 体外 | DMSO | 53 mg/mL (197.21 mM) | |
Ethanol | 10 mg/mL (37.21 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Moclobemide is a MAO-A (5-HT) inhibitor with IC50 of 6.1 μM. |
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in vitro | Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat brain with ED50 of 7.6 μmol/kg and 78 μmol/kg, respectively. Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. Moclobemide (0.1 mM), which inhibits brain MAO-A activity by over 80%, does not affect benzylamine oxidase (rat heart) and diamine oxidase (rat small intestine) activity in vitro. [1] Moclobemide (10 mM-100 mM) includes in the culture medium during anoxia or with glutamate significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex. [2] |
in vivo | Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. [1] Moclobemide, given via the drinking water (4.5 mg/kg/day), produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. Moclobemide upregulates hippocampal mineralocorticoid receptor (MR) levels in rats by 65%, 76% and 19% at 2 weeks, 5 weeks and 7 weeks of treatment, and upregulates Glucocorticoid receptor (GR) levels in this limbic brain structure by 10% at 5 weeks. Moclobemide treatment (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. [3] Moclobemide (2.5 mg/kg/day) decreases immobility and increases climbing behavior following treatment for 3 days, but increases in both swimming and climbing behaviors are measured following treatment for 14 days. Moclobemide (15 mg/kg/day) decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing). [4] Moclobemide (100 mg/kg/day) combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. Moclobemide (100 mg/kg/day) reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats. [5] |
キナーゼアッセイ | Binding assay | |
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20 μL aliquots of the homogenates are preincubated with the inhibitor in a total volume of 220 μL at 37 ℃ for 30 min. At the end of the preincubation period, the enzyme reaction is started by addition of 80 μL of the MAO-A substrate [14C]-5-HT (0.3 mCi/mmol, final concentration 2 × 10-4 M) or of the MAO-B substrate [14C]PEA (8 mCi/mmol; final concentration, 2 × 10-5 M) and the incubation continued for 10 mm at 37 ℃. Then, the reaction is stopped by addition of 200 μL of 2 N HCl, and the deaminated metabolites are extracted by vigorous shaking for 10 min with 5 mL of diethylether (5-HT-extraction) or n-heptane (PEA-extraction). After centrifugation (103 × g 30 sec) the water-phase is frozen in dry ice and the organic layer poured into plastic vials containing 5 mL of scintillation cocktail. Finally, the radioactivity is determined in a scintillation spectrometry. |
Data from [Data independently produced by , , Sci Rep, 2016, 6: 36382.]
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] | PubMed: 34508571 |
Attenuated monoamine oxidase a impairs endometrial receptivity in women with adenomyosis via downregulation of FOXO1 [ Biol Reprod, 2021, ioab182] | PubMed: 34568943 |
Partial reversal of the effort-related motivational effects of tetrabenazine with the MAO-B inhibitor deprenyl (selegiline): Implications for treating motivational dysfunctions. [ Pharmacol Biochem Behav, 2018, 166:13-20] | PubMed: 29309800 |
Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. [Nie T, et al. Sci Rep, 2016, 6:36382] | PubMed: 27805061 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。