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hMAO-B-IN-2

Catalog No. T60678 CAS 2454459-87-9

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].

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hMAO-B-IN-2, CAS 2454459-87-9

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	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.

Molecular Weight	301.38
Formula	C18H23NO3
CAS No.	2454459-87-9

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

hMAO-B-IN-2 2454459-87-9 inhibitor inhibit

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