gamma-secretase modulator 2
Based on 1 publication(s) in Google Scholar
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for study of Alzheimer's disease.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.00%
- CAS 番号: 1093978-89-2
- 分子式: C25H22F4N6O2
- 分子量:514.47
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 gamma-secretase modulator 2
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
12.9 μM
Compound: 34
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Inhibition of human ERG expressed in HEK cells assessed as reduction in IKr current by patchXpress assay
Inhibition of human ERG expressed in HEK cells assessed as reduction in IKr current by patchXpress assay
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[PMID: 26212776] |
| HEK293 | IC50 |
2.61 μM
Compound: 34
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Binding affinity to human ERG expressed in HEK cells by MK-499 radioligand displacement assay
Binding affinity to human ERG expressed in HEK cells by MK-499 radioligand displacement assay
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[PMID: 26212776] |
| HeLa | IC50 |
39.8 μM
Compound: 34
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Inhibition of gamma-secretase-mediated cleavage of NotchdeltaE in human HeLa cells expressing NotchdeltaE assessed as intracellular release of Notch intracellular domain (NICD)/N-terminal luciferase by luminescent method
Inhibition of gamma-secretase-mediated cleavage of NotchdeltaE in human HeLa cells expressing NotchdeltaE assessed as intracellular release of Notch intracellular domain (NICD)/N-terminal luciferase by luminescent method
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[PMID: 26212776] |
| SH-SY5Y | IC50 |
0.03 μM
Compound: 34
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Inhibition of gamma-secretase in human SH-SY5Y cells expressing beta-APP C-terminal fragment SPA4CT assessed as decrease of amyloid beta-42 level by electrochemiluminescent method
Inhibition of gamma-secretase in human SH-SY5Y cells expressing beta-APP C-terminal fragment SPA4CT assessed as decrease of amyloid beta-42 level by electrochemiluminescent method
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[PMID: 26212776] |
| SH-SY5Y | IC50 |
0.13 μM
Compound: 34
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Inhibition of gamma-secretase in human SH-SY5Y cells expressing beta-APP C-terminal fragment SPA4CT assessed as decrease of amyloid beta-40 level by electrochemiluminescent method
Inhibition of gamma-secretase in human SH-SY5Y cells expressing beta-APP C-terminal fragment SPA4CT assessed as decrease of amyloid beta-40 level by electrochemiluminescent method
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[PMID: 26212776] |
化学情報
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CAS 番号 1093978-89-2
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性状 Solid
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分子量 514.47
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分子式 C25H22F4N6O2
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Color White to off-white
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SMILES
O=C1N(C2=CC=CC(F)=C2CCC1N3N=NC(C4=CC(OC)=C(N5C=NC(C)=C5)C=C4)=C3)CC(F)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (194.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
純度とドキュメンテーション
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データシート (248 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9437 mL | 9.7187 mL | 19.4375 mL | 48.5937 mL |
| 5 mM | 0.3887 mL | 1.9437 mL | 3.8875 mL | 9.7187 mL | |
| 10 mM | 0.1944 mL | 0.9719 mL | 1.9437 mL | 4.8594 mL | |
| 15 mM | 0.1296 mL | 0.6479 mL | 1.2958 mL | 3.2396 mL | |
| 20 mM | 0.0972 mL | 0.4859 mL | 0.9719 mL | 2.4297 mL | |
| 25 mM | 0.0777 mL | 0.3887 mL | 0.7775 mL | 1.9437 mL | |
| 30 mM | 0.0648 mL | 0.3240 mL | 0.6479 mL | 1.6198 mL | |
| 40 mM | 0.0486 mL | 0.2430 mL | 0.4859 mL | 1.2148 mL | |
| 50 mM | 0.0389 mL | 0.1944 mL | 0.3887 mL | 0.9719 mL | |
| 60 mM | 0.0324 mL | 0.1620 mL | 0.3240 mL | 0.8099 mL | |
| 80 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6074 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1944 mL | 0.4859 mL |
gamma-secretase modulator 2 関連分類
HY-50754 関連分類
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