1. Neuronal Signaling Stem Cell/Wnt
  2. γ-secretase Amyloid-β
  3. ELND 006

ELND 006(compound 30)是一种代谢稳定的 γ-分泌酶 (γ-secretase) 抑制剂,可选择性抑制淀粉样蛋白β(Aβ)的生成,同时保留 Notch 信号传导。ELND 006 及其类似物 ELND007(compound 34)均在体外和体内有效降低 Aβ 水平。与其他 γ-分泌酶抑制剂(如 Semagacestat、Begacestat 和 Avagacestat)相比,ELND 006 在降低脑脊液 (CSF) 中 Aβ 水平方面的效力显著,对阿尔茨海默病具有潜在的抑制作用。

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ELND 006 Chemical Structure

ELND 006 Chemical Structure

CAS No. : 1333990-84-3

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规格 价格 是否有货 数量
1 mg ¥1300
In-stock
5 mg ¥3285
In-stock
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50 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO ED50
1.1 nM
Compound: 30, ELND006
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
[PMID: 23713656]
CHO IC50
82 nM
Compound: ELND006
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
[PMID: 23312944]
CHO ED50
86 nM
Compound: 30, ELND006
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
[PMID: 23713656]
HEK293 ED50
1.1 nM
Compound: ELND006
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis
[PMID: 23312944]
IMR-32 IC50
0.34 nM
Compound: ELND006
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
[PMID: 23312944]
IMR-32 IC50
5.3 nM
Compound: ELND006
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
[PMID: 23312944]
分子量

455.40

Formula

C20H14F5N3O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (109.79 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1959 mL 10.9794 mL 21.9587 mL
5 mM 0.4392 mL 2.1959 mL 4.3917 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.7%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1959 mL 10.9794 mL 21.9587 mL 54.8968 mL
5 mM 0.4392 mL 2.1959 mL 4.3917 mL 10.9794 mL
10 mM 0.2196 mL 1.0979 mL 2.1959 mL 5.4897 mL
15 mM 0.1464 mL 0.7320 mL 1.4639 mL 3.6598 mL
20 mM 0.1098 mL 0.5490 mL 1.0979 mL 2.7448 mL
25 mM 0.0878 mL 0.4392 mL 0.8783 mL 2.1959 mL
30 mM 0.0732 mL 0.3660 mL 0.7320 mL 1.8299 mL
40 mM 0.0549 mL 0.2745 mL 0.5490 mL 1.3724 mL
50 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0979 mL
60 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9149 mL
80 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL
100 mM 0.0220 mL 0.1098 mL 0.2196 mL 0.5490 mL
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:
ELND 006
目录号:
HY-16632
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