1. Neuronal Signaling
  2. Beta-secretase Amyloid-β
  3. BACE1/2-IN-1

BACE1/2-IN-1 (化合物 34) 是一种有效的 BACE1BACE2 抑制剂,其 IC50 分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 显示了较低的 Pgp 外排比和提高的被动渗透率。BACE1/2-IN-1 显示肝脏微粒体代谢稳定性降低。

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BACE1/2-IN-1 Chemical Structure

BACE1/2-IN-1 Chemical Structure

CAS No. : 2671036-34-1

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查看 Beta-secretase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].

IC50 & Target

IC50: 0.0053 μM (BACE2), 0.01 μM (BACE1), 160 μM (Cathepsin D)[1]

体外研究
(In Vitro)

BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D[1].

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

体内研究
(In Vivo)

BACE1/2-IN-1 (compound 34) (PDAPP (V717F) transgenic mice, 0-100 mg/kg, Subcutaneous injection, once) shows significant reduction in PDAPP mouse cortex Aβ at 100 mg/kg (40%), and 30 mg/kg (24%), but not at 10 mg/kg (12%NS)[1].

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

分子量

401.57

Formula

C21H31N5OS

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

BACE1/2-IN-1 相关分类

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  • 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.

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