δ-Secretase inhibitor 11
目录号 : GC66048
Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.
Cas No.:842964-18-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.
Compound 11 inhibit δ-secretase in Pala cells, with an IC50 of 7?μM. Compounds 11 is highly permeable assessed by Caco-2 monolayer permeability screen. The human liver microsomal stability screen demonstrates that following 30?min of incubation, 76% of compound 11 remained in human liver microsomes.[1]
Chronic treatment with δ-secretase inhibitor 11 markedly decreases the brain asparaginyl endopeptidase (AEP) activity, reduces the generation of Aβ1-40/42 and ameliorates memory loss. The inhibition of AEP with this reagent not only reduces the AEP-cleaved tau fragments and tau hyperphosphorylation, but also attenuates neuroinflammation in the form of microglial activation. Treatment with δ-secretase inhibitor 11 prevents the synaptic loss and alleviated dendritic disruption in senescence-accelerated mouse prone 8 (SAMP8) mouse brain.[2]
[1] Zhang Z, et al. Nat Commun. 2017 Mar 27;8:14740. [2] Wang J, et al. Transl Neurodegener. 2021 Mar 31;10(1):12.
| Cas No. | 842964-18-5 | SDF | Download SDF |
| 分子式 | C10H12N4O2 | 分子量 | 220.23 |
| 溶解度 | DMSO : 125 mg/mL (567.59 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。