Powder: -20°C for 3 years | In solvent: -80°C for 1 year
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible inhibitor of hMAO-B (IC 50 = 4 nM) that can be used for the research of alzheimer’s disease. hMAO-B-IN-2 exhibits good neuroprotective effects and low toxicity in SH-SY5Y cell [1].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 349,000 |
50 mg | 約6-8 週間 | ¥ 454,500 |
100 mg | 約6-8 週間 | ¥ 574,000 |
説明 | hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible inhibitor of hMAO-B (IC 50 = 4 nM) that can be used for the research of alzheimer’s disease. hMAO-B-IN-2 exhibits good neuroprotective effects and low toxicity in SH-SY5Y cell [1]. |
In vitro | hMAO-B-IN-2 (compound 6j), across a range of concentrations (0-100 μM), demonstrates significant inhibitory activity, achieving IC50 values of 4 nM for hMAO-B and 6.04 nM for hMAO-A. Notably, this compound acts as a reversible inhibitor of MAO-B, with enzyme activity largely recoverable after dilution of 6j to 0.1 × IC50 and 1 × IC50, showing approximately 82% and 45% activity restoration, respectively. Additionally, hMAO-B-IN-2, at a concentration of 25 μM over 48 hours, significantly inhibits MAO-B and effectively blocks Aβ self-induced aggregation by 40.78 ± 6.27%. In neuroprotective aspects, hMAO-B-IN-2 promotes cell survival in a dose-dependent manner without exhibiting toxicity at concentrations up to 25 μM over 24 hours, as evaluated in SH-SY5Y neuroblastoma cells, emphasizing its potential against neurodegenerative diseases. |
In vivo | Compound hMAO-B-IN-2 (6j), administered to male Sprague-Dawley rats at doses of 3 mg/kg intravenously (IV) and 10 mg/kg orally (PO), exhibits satisfactory pharmacokinetic properties, including a high peak concentration (Cmax), a suitable half-life (T 1/2), and favorable oral bioavailability (F%). Specifically, the intravenous administration resulted in a peak concentration of 639.29 ± 89.06 μg/L, a half-life of approximately 1.02 ± 0.17 hours, and a clearance rate of 3.33 ± 0.15 L/h/kg. Oral administration showed a peak concentration of 142.17 ± 72.21 μg/L, a half-life of 1.33 ± 0.16 hours, and an oral bioavailability of 36.10%. These findings underscore the compound's efficacy and its potential for further pharmacological development. |
分子量 | 301.38 |
分子式 | C18H23NO3 |
CAS No. | 2454459-87-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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hMAO-B-IN-2 2454459-87-9 Inhibitor inhibitor inhibit