MAO-IN-M30 dihydrochloride 是一种口服活性，可通过血脑屏障的，脑选择性不可逆MAO-A(IC50=37 nM) 和MAO-B(IC50=57 nM) 抑制剂。MAO-IN-M30 dihydrochloride 是有效的铁螯合剂、自由基清除剂。MAO-IN-M30 dihydrochloride 对 Dexamethasone 诱导的脑细胞凋亡具有神经保护作用。MAO-IN-M30 dihydrochloride 在 MPTP 和 lactacystin 帕金森病模型中也显示出神经恢复活性。
| 生物活性 | MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversibleMAO-A(IC50=37 nM) andMAO-B(IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potentiron chelatorandradical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cellapoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease[1][2][3]. |
| IC50& Target[1] | MAO-A 37 nM (IC50) | MAO-B 57 nM (IC50) |
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体外研究
(In Vitro) | MAO-IN-M30 (0.25 nM; 72 hours) significantly increased cell viability to ~90% after exposure to Dexamethasone[3].
MAO-IN-M30 (0-10 μM; 24 hours) enhances PC12 cell survival[4].
MAO-IN-M30 treatment significantly decreases the occurrence of fragmented DNA compared to the dexamethasone-treated group in SH-SY5Y cells[3].
Cell Viability Assay[3] | Cell Line: | SH-SY5Y cells | | Concentration: | 0.25 nM | | Incubation Time: | 72 hours | | Result: | Significantly increased cell viability to ~90% after exposure to Dexamethasone. |
Cell Viability Assay[4] | Cell Line: | PC12 cells | | Concentration: | 0-10 μM | | Incubation Time: | 24 hours | | Result: | Enhanced the PC12 cell viability, the cell viability increasing to 85 ± 6 and 90 ± 7%. |
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体内研究
(In Vivo) | MAO-IN-M30 (0.5-2.5 mg/kg; p.o.; once daily for 14 consecutive days) possesses neuroprotective activities[6].
| Animal Model: | Male C57/BL mice (20-22 g; MPTP-induced neurotoxicity in mice)[6] | | Dosage: | 0.5, 2.5 mg/kg | | Administration: | P.o.; once daily for 14 consecutive days | | Result: | Significantly elevate striatal dopamine levels, reduce its metabolism, and elevate tyrosine-hydroxylase protein levels and activity. Elevated MPTP-reduced dopaminergic and transferrin receptor cell count in the SNpc. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 2 mg/mL(6.68 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.3422 mL | 16.7112 mL | 33.4225 mL | | 5 mM | 0.6684 mL | 3.3422 mL | 6.6845 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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