GSM-1
Based on 1 Customer Validation
GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
For research use only. We do not sell to patients.
- Purity: 98.41%
- CAS No.: 884600-68-4
- Formula: C26H31ClF3NO2
- Molecular Weight:481.98
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
68 nM
Compound: GSM-1
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Modulation of gamma-secretase expressed in CHO cells co-expressing wild type APP and PS1 assessed as inhibition of amyloid beta-42 production sandwich ELISA
Modulation of gamma-secretase expressed in CHO cells co-expressing wild type APP and PS1 assessed as inhibition of amyloid beta-42 production sandwich ELISA
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[PMID: 23000293] |
| HEK293 | IC50 |
120 nM
Compound: GSM-1
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Modulation of gamma-secretase in HEK293 cells transfected with APPsw-6myc assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
Modulation of gamma-secretase in HEK293 cells transfected with APPsw-6myc assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
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[PMID: 26142947] |
| HEK293 | IC50 |
120 nM
Compound: 2
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Modulation of gamma-secretase (unknown origin) expressed in HEK293 cells assessed as reduction of amyloid beta 42 level
Modulation of gamma-secretase (unknown origin) expressed in HEK293 cells assessed as reduction of amyloid beta 42 level
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[PMID: 24428186] |
GSM-1 increases the levels of Aβ38 produced from WT APP. GSM-1 potently loweres the levels of Aβ42 of WT APP and all the Phe mutants by ～70–80%, even for the V44F mutant, which produced only extremely small amounts of Aβ42[1].
GSM-1 directly binds to the N-terminal fragment of PS1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 884600-68-4
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Appearance Solid
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Molecular Weight 481.98
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Formula C26H31ClF3NO2
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Color Light yellow to yellow
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SMILES
O=C(O)C[C@H]1C[C@@H](C2=CC=C(C(F)(F)F)C=C2)N([C@@H](C3=CC=C(Cl)C=C3)CCC(C)C)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (207.48 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Richard M, et al. Beta-amyloid Precursor Protein Mutants Respond to Gamma-Secretase Modulators. J Biol Chem. 2010 Jun 4;285(23):17798-810. [Content Brief]
[2]. Yu Ohki, et al. Phenylpiperidine-type γ-secretase Modulators Target the Transmembrane Domain 1 of Presenilin 1. EMBO J. 2011 Oct 14;30(23):4815-24. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0748 mL | 10.3739 mL | 20.7477 mL | 51.8694 mL |
| 5 mM | 0.4150 mL | 2.0748 mL | 4.1495 mL | 10.3739 mL | |
| 10 mM | 0.2075 mL | 1.0374 mL | 2.0748 mL | 5.1869 mL | |
| 15 mM | 0.1383 mL | 0.6916 mL | 1.3832 mL | 3.4580 mL | |
| 20 mM | 0.1037 mL | 0.5187 mL | 1.0374 mL | 2.5935 mL | |
| 25 mM | 0.0830 mL | 0.4150 mL | 0.8299 mL | 2.0748 mL | |
| 30 mM | 0.0692 mL | 0.3458 mL | 0.6916 mL | 1.7290 mL | |
| 40 mM | 0.0519 mL | 0.2593 mL | 0.5187 mL | 1.2967 mL | |
| 50 mM | 0.0415 mL | 0.2075 mL | 0.4150 mL | 1.0374 mL | |
| 60 mM | 0.0346 mL | 0.1729 mL | 0.3458 mL | 0.8645 mL | |
| 80 mM | 0.0259 mL | 0.1297 mL | 0.2593 mL | 0.6484 mL | |
| 100 mM | 0.0207 mL | 0.1037 mL | 0.2075 mL | 0.5187 mL |
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