1. Apoptosis Neuronal Signaling
  2. Caspase Amyloid-β
  3. δ-Secretase inhibitor 11

δ-Secretase inhibitor 11 

目录号: HY-124832 纯度: 99.06%
COA 产品使用指南

δ-Secretase inhibitor 11 (compound 11) 是一种口服有效、可透过血脑屏障的、无毒、选择性和特异性的 δ-secretase 抑制剂,其 IC50 为 0.7 μM。δ-Secretase inhibitor 11 与 δ-Secretase 的活性位点和变构位点相互作用。δ-Secretase inhibitor 11 可衰减 tau 和 APP (淀粉样前体蛋白)的裂解。δ-Secretase inhibitor 11 可改善tau P301S 和 5XFAD 转基因小鼠模型的突触功能障碍和认知功能障碍。δ-Secretase inhibitor 11 可用于阿尔茨海默病的研究。

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δ-Secretase inhibitor 11 Chemical Structure

δ-Secretase inhibitor 11 Chemical Structure

CAS No. : 842964-18-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].

IC50 & Target

Caspase-3

31.86 ± 1. μM (IC50)

Caspase-8

86.71 ± 10 μM (IC50)

体外研究
(In Vitro)

δ-Secretase inhibitor 11 (化合物 11) (0-1 μM,10 分钟) 以浓度和时间依赖性方式抑制 δ-分泌酶[1]
δ-Secretase inhibitor 11 (0-1 μM) 通过 δ-分泌酶选择性地阻断 tau 和 APP (淀粉样前体蛋白) 片段化[1]

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

体内研究
(In Vivo)

δ-Secretase inhibitor 11 (化合物 11) (10 mg/kg,口服,每天一次,持续 3 个月) 减轻 OGD (氧糖剥夺) 诱导的神经元损伤,并特别发挥神经保护作用[1]
δ-Secretase inhibitor 11 (0-10 mg/kg,口服,每天一次,持续 1.5 个月和 3 个月) 抑制 δ-分泌酶活性,减轻 5XFAD 小鼠模型中的 Aβ 沉积和认知缺陷[1]

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

Animal Model: Tau P301S transgenic mice (n=4 mice per group)[1]
Dosage: 10 mg/kg
Administration: Orally, once daily for 3 months
Result: Significantly inhibited the activity of δ-secretase in both wild-type and tau P301S mice brain, increased PP2A activity, and attenuated the truncation and phosphorylation of tau in tau P301S mice. Ameliorated synaptic loss and restored synaptic dysfunction in tau P301S mice.
Animal Model: 5XFAD mice[1]
Dosage: 2, 5 or 10 mg kg
Administration: Orally, once daily for 1.5 and 3 months
Result: Attenuated the β-secretase-mediated processing of APP, significantly decreased the concentrations of Aβ 1-40 and Aβ 1-42 in the brain lysates, and attenuated Aβ deposition in a time- and dose-dependent manner.
分子量

220.23

Formula

C10H12N4O2

CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (567.59 mM; 超声助溶; 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 4.5407 mL 22.7035 mL 45.4071 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 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 (protect from light)。-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
参考文献

δ-Secretase inhibitor 11 相关分类

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 (protect from light)。-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 4.5407 mL 22.7035 mL 45.4071 mL 113.5177 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 mL 22.7035 mL
10 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
15 mM 0.3027 mL 1.5136 mL 3.0271 mL 7.5678 mL
20 mM 0.2270 mL 1.1352 mL 2.2704 mL 5.6759 mL
25 mM 0.1816 mL 0.9081 mL 1.8163 mL 4.5407 mL
30 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7839 mL
40 mM 0.1135 mL 0.5676 mL 1.1352 mL 2.8379 mL
50 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
60 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
80 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4190 mL
100 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 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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δ-Secretase inhibitor 11
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HY-124832
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