2. Neuronal Signaling
  3. Cholinesterase (ChE) Amyloid-β
  4. hAChE/hBACE-1-IN-4

hAChE/hBACE-1-IN-4 (化合物 AK-2) 是一种喹唑啉衍生物，hAChE/hBACE-1-IN-4 对 hAChE 和 hBACE-1 酶表现出良好且显著的抑制活性 (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM) 和抑制 Aβ 聚集的潜力，具有血脑屏障通透性和口服活性，且不具有神经毒性。hAChE/hBACE-1-IN-4 可用于阿尔兹海默病的研究。

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hAChE/hBACE-1-IN-4 Chemical Structure

hAChE/hBACE-1-IN-4 Chemical Structure

CAS No. : 229476-71-5

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hAChE/hBACE-1-IN-4 相关抗体

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查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research[1].

IC50 & Target[1]

hAChE

0.283 μM (IC50)

hBCHE

0.231 μM (IC50)

体外研究
(In Vitro)

hAChE/hBACE-1-IN-4 (10，20，40 和 80 μM；24 h) 具有非神经毒性[1]。

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

hAChE/hBACE-1-IN-4 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y
Concentration: 10, 20, 40 and 80 μM
Incubation Time: 24 h
Result: Reduced cell viability by 26% at maximum concentration (80 μM).
体内研究
(In Vivo)

hAChE/hBACE-1-IN-4 (500 mg/kg，口服， 14 天) 具有很大的安全边际在 Wistar 大鼠体内，可以安全地用于进一步的体内研究[1]。
hAChE/hBACE-1-IN-4 (500 mg/kg，口服， 9 天) 抑制 BACE-1 活性来恢复认知缺陷，在测试剂量下具有抗 aβ 药物的作用在 Wistar 大鼠体内[1]。
hAChE/hBACE-1-IN-4 (500 mg/kg，灌胃， 4 天) 具有穿过血脑屏障的能力，达到其在脑组织中的特定作用部位发挥作用[1]。

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

Animal Model: Wistar rats [1]
Dosage: 500 mg/kg for 14 days
Administration: Oral gavage (p.o.)
Result: Observed the renal and hepatic functional parameters within the prescribed limits
. Examined and found with normal tissue appearance such as kidneys, heart, liver, and brains.
Animal Model: Wistar rats [1]
Dosage: 20mg/kg for 9 days
Administration: Oral gavage (p.o.)
Result: Decreased the ELT and increased total platform crossing as compared to the diseased model group
. Increased the neuronal density and neuronal arrangement.
Animal Model: Wistar rats[1]
Dosage: 10 and 20 mg/kg for 4 days
Administration: i.g.
Result: The concentrations of AK-2 in brain homogenates were observed to 0.633 and 0.977 μg/mL.
分子量

364.44

Formula

C21H24N4O2
CAS 号
Unlabeled Cas

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

hAChE/hBACE-1-IN-4 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

hAChE/hBACE-1-IN-4229476-71-5Cholinesterase (ChE)Amyloid-ββ-amyloid peptideAβAbetahAChE/hBACE InhibitorAlzheimer’s diseaseWistar ratsInhibitorinhibitorinhibit

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