1. Neuronal Signaling
  2. Beta-secretase
  3. AM-6494

AM-6494 是一种有效的口服 β-位点淀粉样前体蛋白裂解酶 1 (BACE1) 抑制剂 (IC50=0.4 nM),体内选择性高于 BACE2 (IC50=18.6 nM)。AM-6494 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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AM-6494 Chemical Structure

AM-6494 Chemical Structure

CAS No. : 1874232-80-0

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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

AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM)[1]. AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

BACE1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
137 μM
Compound: 20; AM-6494
Inhibition of recombinant CatD (unknown origin) expressed in CHO cells using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET assay
Inhibition of recombinant CatD (unknown origin) expressed in CHO cells using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET assay
[PMID: 31589043]
HEK293 IC50
1.2 nM
Compound: 20; AM-6494
Inhibition of BACE in HEK293 cells harboring APP Swedish mutant assessed as reduction in amyloid beta 40 level measured after overnight incubation by sandwich ELISA
Inhibition of BACE in HEK293 cells harboring APP Swedish mutant assessed as reduction in amyloid beta 40 level measured after overnight incubation by sandwich ELISA
[PMID: 31589043]
HEK293 IC50
569 nM
Compound: 20; AM-6494
Inhibition of recombinant human BACE2 expressed in HEK293 cells co-transfected with N-terminal HA-tagged/C-terminal Myc tagged Mbeta chain of human PMEL17 measured after overnight incubation by Gaussia luciferase reporter gene assay
Inhibition of recombinant human BACE2 expressed in HEK293 cells co-transfected with N-terminal HA-tagged/C-terminal Myc tagged Mbeta chain of human PMEL17 measured after overnight incubation by Gaussia luciferase reporter gene assay
[PMID: 31589043]
分子量

473.50

Formula

C22H21F2N5O3S

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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  • 稀释计算器

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Help & FAQs
  • 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:
AM-6494
目录号:
HY-128774
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