1. Neuronal Signaling Metabolic Enzyme/Protease
  2. Beta-secretase Cathepsin Amyloid-β
  3. NB-533

NB-533 是一种具有口服活性且可穿透血脑屏障的 BACE-1 抑制剂,对人源靶点的 IC50 为 0.002 μM。NB-533 还可抑制人源组织蛋白酶 D (cathepsin D),其 IC50 为 0.001 μM。NB-533 可抑制产淀粉样蛋白的淀粉样前体蛋白 (APP) 加工过程,并减少 40 的释放。NB-533 可降低转基因小鼠脑内 APP 代谢产物 C99 和 Aβ40 的水平。NB-533 可用于阿尔茨海默病的研究。

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NB-533

NB-533 Chemical Structure

CAS No. : 1146544-18-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces 40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease[1].

IC50 & Target[1]

BACE1

0.002 μM (IC50)

Cathepsin D

0.001 μM (IC50)

体外研究
(In Vitro)

NB-533 可强效抑制人源 BACE-1 酶,其 IC50 为 0.002 μM[1]
NB-533 可抑制人源 APP 转染 CHO 细胞释放 Aβ40,其 IC50 为 0.024 μM[1]
NB-533 以 0.001 μM 的 IC50 值抑制人组织蛋白酶 D[1]
NB-533 在 MDCK mdr1a 细胞中的外排率 (BA/AB) 为 9.4,显示出对 P-糖蛋白的敏感性降低[1]

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

体内研究
(In Vivo)

NB-533 (100 μmol/kg;口服;于 0 小时和 3 小时给药两次) 可使 APP51/16 转基因小鼠的前脑 C99 水平显著降低 20%,脑脊液 Aβ40 水平显著降低 26%[1]

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

Animal Model: APP51/16 transgenic mice (expressing wild-type human APP under a brain-specific promoter)[1]
Dosage: 100 μmol/kg
Administration: p.o.; at 0 and 3 hours
Result: Reached brain levels of 0.53 μmol/kg, with no detectable effect on measured endpoints.
Reached brain levels of 1.5 μmol/kg, resulting in a significant 20% reduction in forebrain C99 and a significant 26% reduction in CSF Aβ40; no significant reduction in brain Aβ40 was observed.
分子量

557.81

Formula

C33H55N3O4

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
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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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产品名称:
NB-533
目录号:
HY-182429
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