2. Neuronal Signaling Stem Cell/Wnt PI3K/Akt/mTOR
  3. Beta-secretase Cholinesterase (ChE) GSK-3
  4. AChE/BACE1/GSK3β-IN-1

AChE/BACE1/GSK3β-IN-1 是 AChE/BACE1/GSK3β 的三重抑制剂，具有口服活性。AChE/BACE1/GSK3β- IN -1 对AChE、BACE1 和 GSK3β 均有抑制活性，其 IC50 值分别为 1.0 μM、20 μM 和 15 μM。AChE/BACE1/GSK3β-IN-1 具有良好的血脑屏障穿透性，生物利用度适中。AChE/BACE1/GSK3β-IN-1 可用于阿尔茨海默 (AD) 的研究。

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AChE/BACE1/GSK3β-IN-1 Chemical Structure

AChE/BACE1/GSK3β-IN-1 Chemical Structure

CAS No. : 2866066-81-9

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AChE/BACE1/GSK3β-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Beta-secretase 亚型特异性产品:

查看所有亚型
BACE1 BACE2

查看 Cholinesterase (ChE) 亚型特异性产品:

查看所有亚型
AChE BChE

查看 GSK-3 亚型特异性产品:

查看所有亚型
GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD)[1].

IC50 & Target[1]

BACE1

20 μM (IC50)

AChE

1 μM (IC50)

GSK-3β

15 μM (IC50)

体外研究
(In Vitro)

AChE/BACE1/GSK3β-IN-1 shows effective inhibition for AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively[1].
AChE/BACE1/GSK3β-IN-1 can pass through BBB[1].

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

AChE/BACE1/GSK3β-IN-1 相关抗体:
体内研究
(In Vivo)

AChE/BACE1/GSK3β-IN-1 (oral, 200 and 400 mg/kg, single) shows no acute toxicity and good safety profile in C57B6/J Mice[1].
AChE/BACE1/GSK3β-IN-1 (p.o., 100 mg/kg; i.v., 10 mg/kg)has good PK profiles[1].
AChE/BACE1/GSK3β-IN-1 (gavage, 2.5 mg/kg, 5 mg/kg and 10mg/kg, for 7 consecutive days) can ameliorate the impaired learning and memory in Aβ-induced AD mice[1].
AChE/BACE1/GSK3β-IN-1 inhibits the expression of ADAM17 in the cortex and significantly decreases the expressions of ADAM17 and BACE1 in AD mice[1].

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

Animal Model: C57B6/J Mice[1]
Dosage: 200 and 400 mg/kg
Administration: oral, single
Result: Increased slightly serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST), but no significant difference.
Showed no significant change in the content of blood urea nitrogen (BUN).
Did not change significantly the morphology of liver and kidney tissue of mice.
Animal Model: male Sprague-Dawley (SD) rats[1]
Dosage: 10 mg/kg and 100 mg/kg
Administration: oral and intravenous
Result:
parameters 100 mg/kg (p.o.) 10 mg/kg(i.v.)
Cmax(ng/mL) 167 ± 13 2796 ± 259
AUC0−t(ng/mL) 1010 ± 112 1031 ± 86
AUC0−∞(ng/mL*h) 1635 ± 362 1047 ± 88
t1/2 (h) 20 ± 9 0.4 ± 0.04
Cl (L/h/kg) 63 ± 12 10 ± 1
MRT0−∞(h) 26 ± 11 0.3 ± 0
VZ(L/kg) 1730 ± 387 5 ± 1
Tmax(h) 1 0.08
F (%) 9.8
Animal Model: Aβ-induced AD mice[1]
Dosage: 2.5 mg/kg, 5 mg/kg and 10mg/kg
Administration: gavage, for 7 consecutive days
Result: Decreased the escape latency of mice.
Increased the number of crossing platforms in mice in a dose-dependent trend.
分子量

450.50

Formula

C26H27FN2O4
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

AChE/BACE1/GSK3β-IN-1 相关分类

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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:

AChE/BACE1/GSK3β-IN-12866066-81-9Beta-secretaseCholinesterase (ChE)GSK-3BACEβ-Secretase Glycogen synthase kinase-3Glycogen synthase kinase 3oralAChEBACE1GSK3βblood-brain barrierbioavailabilityAlzheimer's disease (AD)Inhibitorinhibitorinhibit

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