| 产品描述: | MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent. |
| 体外研究: |
MAO-A/5-HT2AR-IN-1 (compound I14) (0-4 μM, 24 h) exhibits a significant neurocytoprotective effect on the CORT-induced cell depression model. MAO-A/5-HT2AR-IN-1 is able to occupy the active cavity of 5-HT2AR and MAO-A with multiple hydrogen bonding forces and π–π stacking interaction. MAO-A/5-HT2AR-IN-1 exhibits low proliferation inhibitory activities against L02 cells (IC50 > 100 μM), SH-SY5Y (IC50 > 10 μM) and PC12 (IC50 > 10 μM), indicating it has a good safety profile. |
| 体内研究: |
MAO-A/5-HT2AR-IN-1 (compound I14) (10 and 20 mg/kg) significantly ameliorates the depression-like behavior of mice. MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion and the depression-like behavior. MAO-A/5-HT2AR-IN-1 is able t 웿 Ů ñ 샮㡽䇘睜⪰ޏࠃ 䇩睜 䇩睜Ȃ Ӥ 晐睦Ӥ 晐睦Ӥ 峀睜 弴睜 ڤ 犐ƈ ڤ郥댻嬧睜Ӥ 乨Ƥ鄩댻婯睜Љ �ޝ乜Ƥ媜 |
| 参考文献: |
1. Sun X, Li N, et al. Development of MAO-A and 5-HT2AR Dual Inhibitors with Improved Antidepressant Activity. J Med Chem. 2022 Oct 13;65(19):13385-13400.
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| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.077 ml |
10.383 ml |
20.766 ml |
| 5 mM |
0.415 ml |
2.077 ml |
4.153 ml |
| 10 mM |
0.208 ml |
1.038 ml |
2.077 ml |
| 50 mM |
0.042 ml |
0.208 ml |
0.415 ml |
|
| 注意: |
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