1. Neuronal Signaling
  2. Cholinesterase (ChE) Beta-secretase Amyloid-β
  3. hAChE/hBACE-1-IN-2

hAChE/hBACE-1-IN-2 是一种有效的,具有口服活性的,可透过血脑屏障的 hAChE/hBChE/hBACE-1 三重抑制剂,IC50 值分别为 0.113 μM, 1.48 μM 和 0.38 μM。hAChE/hBACE-1-IN-2 具有抗氧化活性。hAChE/hBACE-1-IN-2 也抑制 Aβ11-42 聚集。hAChE/hBACE-1-IN-2 可用于研究阿尔茨海默症。

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hAChE/hBACE-1-IN-2 Chemical Structure

hAChE/hBACE-1-IN-2 Chemical Structure

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查看 Cholinesterase (ChE) 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC50s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease[1].

IC50 & Target

hAChE

0.113 μM (IC50)

hBACE-1

0.38 μM (IC50)

hBCHE

1.48 μM (IC50)

体外研究
(In Vitro)

hAChE/hBACE-1-IN-2 (compound 5f) (10-80 μM, 72 h) 在 SH-SY5Y 神经母细胞瘤细胞系中的安全性被认为与 Donepezil (HY-14566) 相似[1]
hAChE/hBACE-1-IN-2 (compound 5f) (20 μM; 48 h, 72 h) 在 SH-SY5Y 神经母细胞瘤细胞系中具有抗 Aβ1-42 聚集电位的潜能[1]

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

Cell Viability Assay[1]

Cell Line: SH-SY5Y cell lines (The SH-SY5Y cells were sequentially treated with RA and BDNF for 6 days)
Concentration: 10, 20, 40, and 80 μM
Incubation Time: 48-72 h
Result: Indicated a similar reduction in the differentiated neuroblastoma cell population at a maximum 80 μM concentration.

Cell Viability Assay[1]

Cell Line: 1-42 treated SH-SY5Y cells (incubated with Aβ1-42 (10μM) for 24 h)
Concentration: 20 μM
Incubation Time: 48-72 h
Result: The cells incubated the cell viability to 65% and 75% after 48 h and 72 h.
体内研究
(In Vivo)

hAChE/hBACE-1-IN-2 (2.5-10 mg/kg,口服, 14 天) 在 Scopolamine (HY-N0296) 诱导的认知缺陷小鼠模型中改善小鼠学习和记忆能力,减少 RTL 和张开双臂的时间[1]
hAChE/hBACE-1-IN-2 ( 500 mg/kg,口服, 14 天) 在瑞士白化小鼠中耐受良好,没有明显毒性,包括大脑,肝脏,肾脏和心脏均没有异常[1]
hAChE/hBACE-1-IN-2 (10 mg/kg,口服, 14 天) 在 Scopolamine (HY-N0296) 诱导的小鼠模型中能够透过血脑屏障,降低海马和皮层脑匀浆中 AchE 水平或底物水解,延缓氧化应激和降低促炎细胞因子水平的潜力[1]
hAChE/hBACE-1-IN-2 (10 mg/kg,口服, 14天) 在 Aβ 诱导的模型中抑制 BACE-1、 Aβ、 APP/Aβ 和 tau 蛋白水平,保护不同脑区的脑组织[1]

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

Animal Model: Swiss albino mice[1]
Dosage: 500 mg/kg
Administration: Oral administration (p.o.), 14 days
Result: Showed no signs or symptoms of toxicity over the 14 days
Animal Model: Scopolamine-induced cognitive deficit mouse model[1]
Dosage: 2.5 mg, 5 mg, and 10 mg/kg
Administration: Oral administration (p.o.), 14 days
Result: Elevated plus maze test showed significant reductions in transfer latency and time spent in open arms, similar to the effects observed with Scopolamine (HY-N0296)-induced dementia reversal.
分子量

408.52

Formula

C22H24N4O2S

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • 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.

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产品名称:
hAChE/hBACE-1-IN-2
目录号:
HY-149288
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