hMAO-B-IN-2 (compound 6j) 是一种口服有效的、选择性的、可穿透血脑屏障的和竞争性可逆hMAO-B抑制剂，其IC50为 4 nM。hMAO-B-IN-2 对 SH-SY5Y 细胞毒性低，具有良好的神经保护作用。hMAO-B-IN-2 可用于研究阿尔茨海默症。
| 生物活性 | hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversiblehMAO-Binhibitor, with anIC50of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research[1]. |
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体外研究
(In Vitro) | hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC50values of 4 nM (hMAO-B) and 6.04 nM (hMAO-A), respectively[1].
hMAO-B-IN-2 (30 min) is a reversible MAO-B inhibitor, the activity of MAO-B enzyme was restored to about 82% and 45% after compound 6j dilution to 0.1 × IC50and 1 ×50, respectively[1].
hMAO-B-IN-2 (25 μM, 48 h) exhibits remarkable inhibitory activities against MAO-B, had good inhibition property of Aβ self-induce aggregation (40.78 ± 6.27%)[1].
hMAO-B-IN-2 (0-100 μM, 24 h) shows non-toxic at the concentrations of 25 μM[1].
hMAO-B-IN-2 (0-25 μM, 24 h) has neuroprotective capability against neurodegeneration disease, and increases cell survival rates in a dose-dependent manner[1].
Cell Cytotoxicity Assay | Cell Line: | SH-SY5Y neuroblastoma cell[1] | | Concentration: | 0, 6.25, 12.5, 25, 50, 100 μM | | Incubation Time: | 24 h | | Result: | Showed non-toxic at the concentrations of 25 μM. |
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体内研究
(In Vivo) | hMAO-B-IN-2 (compound 6j) (Sprague-Dawley rats; 3 mg/kg, IV; 10 mg/kg, PO; once) has acceptable pharmacokinetic properties[1].
Pharmacokinetic Parameters of hMAO-B-IN-2 in male Sprague-Dawley rats[1].
| Parameters | IV (3 mg/kg) | PO (10 mg/kg) | | T1/2(h) | 1.02 ± 0.17 | 1.33 ± 0.16 | | Tmax(h) | | 0.3 | | Cmax(μg/L) | 639.29 ± 89.06 | 142.17 ± 72.21 | | AUC0-inf(μg/L*h) | 247.74 ± 11.48 | 268.49 ± 69.72 | | CL (L/h/kg) | 3.33 ± 0.15 | | | F (%) | | 36.10% |
| Animal Model: | Sprague-Dawley rats (male, 220±20 g)[1] | | Dosage: | 3 mg/kg (IV), 10 mg/kg (PO) | | Administration: | IV, PO (Pharmacokinetic Analysis) | | Result: | Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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