FRM-024
Based on 1 Customer Validation
FRM-024 is a central nervous system-penetrant, orally active γ-secretase modulator and Aβ42 lowering agent. FRM-024 is used for the research of familial Alzheimer's disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.45%
- No. CAS: 2085780-87-4
- Fòrmula: C22H22ClN5O2
- Peso molecular:423.90
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
FRM-024 (Compound 41) potently reduces the level of Aβ42 in H4 cells overexpressing wild-type human APP751, with an EC50 of 9 nM, and also exhibits favorable metabolic stability[1].
FRM-024 inhibits hERG channels in vitro with an IC50 value of 12 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Vss | CL | AUClast | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 30 mg/kg | p.o. | / | / | / | 11,600 nM·h | 754 nM | 86 % |
| Rat[1] | 1 mg/kg | i.v. | 8.7 h | 2.4 L/kg | 3.1 mL/min/kg | / | / | / |
| Dog[1] | 10 mg/kg | p.o. | / | / | / | 32,900 nM·h | 4030 nM | 66 % |
| Dog[1] | 0.5 mg/kg | i.v. | 2.9 h | 0.8 L/kg | 3.4 mL/min/kg | / | / | / |
| Monkey[1] | 30 mg/kg | p.o. | / | / | / | 55,900 nM·h | 6090 nM | 113 % |
| Monkey[1] | 1 mg/kg | i.v. | 3.9 h | 1.2 L/kg | 3.5 mL/min/kg | / | / | / |
Chemical Information
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No. CAS 2085780-87-4
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Appearance Solid
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Peso molecular 423.90
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Fòrmula C22H22ClN5O2
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Color Off-white to light yellow
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SMILES
ClC1=CC=C(C=C1)[C@H]2[C@@H](C3CC3)ON=C(C4=CC=C(N5C=C(N=C5)C)C(OC)=N4)N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvente y solubilidad
DMSO : 100 mg/mL (235.90 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (7.08 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.90 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light, stored under nitrogen). 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 | 2.3590 mL | 11.7952 mL | 23.5905 mL | 58.9762 mL |
| 5 mM | 0.4718 mL | 2.3590 mL | 4.7181 mL | 11.7952 mL | |
| 10 mM | 0.2359 mL | 1.1795 mL | 2.3590 mL | 5.8976 mL | |
| 15 mM | 0.1573 mL | 0.7863 mL | 1.5727 mL | 3.9317 mL | |
| 20 mM | 0.1180 mL | 0.5898 mL | 1.1795 mL | 2.9488 mL | |
| 25 mM | 0.0944 mL | 0.4718 mL | 0.9436 mL | 2.3590 mL | |
| 30 mM | 0.0786 mL | 0.3932 mL | 0.7863 mL | 1.9659 mL | |
| 40 mM | 0.0590 mL | 0.2949 mL | 0.5898 mL | 1.4744 mL | |
| 50 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1795 mL | |
| 60 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9829 mL | |
| 80 mM | 0.0295 mL | 0.1474 mL | 0.2949 mL | 0.7372 mL | |
| 100 mM | 0.0236 mL | 0.1180 mL | 0.2359 mL | 0.5898 mL |
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