2. Neuronal Signaling
  3. Beta-secretase
  4. BACE1-IN-5

BACE1-IN-5 (Compound 15) 是一种 BACE1 抑制剂，IC50 为 9.1 nM，并且还抑制细胞 Aβ，IC50 为 0.82 nM。BACE1-IN-5 具有改善 hERG 抑制和 P-gp 外排的活性分子化学作用。

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BACE1-IN-5 Chemical Structure

BACE1-IN-5 Chemical Structure

CAS No. : 2581114-83-0

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BACE1-IN-5 相关抗体

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查看 Beta-secretase 亚型特异性产品:

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BACE1 BACE2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux[1].

IC50 & Target

BACE1

 

体内研究
(In Vivo)

BACE1-IN-5 (Compound 15; 1-3 mg/kg; oral administration; for 2-6 hours; male ICR mice) treatment results in a significant and dose-dependent decrease of total Aβ, reduces total Aβ by 76% (4 hours) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. BACE1-IN-5 demonstrats a Kp,uu value of 1.3 at 1 mg/kg (4 hours time point). At 3 mg/kg, a maximum Aβ reduction of 87% is achieved at a free brain concentration of 9.5 ng/mL (21 nM) [1].

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

Animal Model: Male ICR mice[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: Oral administration; for 2 hours, 4 hours, and 6 hours
Result: A significant and dose-dependent decrease of total Aβ was seen, reduced total Aβ by 76% (4 h) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. Demonstrats a Kp,uu value close to 1 (Kp,uu of 1.3) at 1 mg/kg (4 h time point). At 3 mg/kg, a maximum Aβ reduction of 87% was achieved at a free brain concentration of 9.5 ng/mL (21 nM).
分子量

461.41

Formula

C18H16F5N5O2S
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

BACE1-IN-5 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

BACE1-IN-52581114-83-0Beta-secretaseBACEβ-SecretaseInhibitorinhibitorinhibit

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