2. Neuronal Signaling
  3. Monoamine Oxidase
  4. hMAO-B-IN-2

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。hMAO-B-IN-2 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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hMAO-B-IN-2 Chemical Structure

hMAO-B-IN-2 Chemical Structure

CAS No. : 2454459-87-9

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hMAO-B-IN-2 相关抗体

Top Publications Citing Use of Products

查看 Monoamine Oxidase 亚型特异性产品:

查看所有亚型
MAO-A MAO-B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 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]. hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

MAO-B

4 nM (IC50)

体外研究
(In Vitro)

hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC50 values 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 × IC50 and 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

hMAO-B-IN-2 相关抗体:

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.
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%

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

301.38

Formula

C18H23NO3
CAS 号
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.
纯度 & 产品资料
参考文献

hMAO-B-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

hMAO-B-IN-22454459-87-9Monoamine OxidaseMAOLow toxicityBlood-brain barrierNeuroprotectiveAlzheimer’s diseaseOrally activeInhibitorinhibitorinhibit

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