MA-0204
Based on 1 Customer Validation
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.31%
- No. CAS: 2095128-17-7
- Fòrmula: C25H27F3N2O4
- Peso molecular:476.49
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Almacenamiento: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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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
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Actividad biológica
Descripciòn
IC50 & Target
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PPARδ 0.4 nM (EC50, in human) |
PPARδ 7.9 nM (EC50, in mouse) |
PPARδ 10 nM (EC50, in rat) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
10 μM
Compound: 2c; MA-0204
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Inhibition of human ERG expressed in HEK293 cells by semi-automatic patch clamp assay
Inhibition of human ERG expressed in HEK293 cells by semi-automatic patch clamp assay
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[PMID: 31889664] |
In Vitro
MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. MA-0204 exhibits high protein binding to mouse plasma, good permeability and low potential for efflux. C[1].
MA-0204 (1.2-12 nM) improves fatty acid oxidation in DMD patient muscle myoblasts mice[1].
MA-0204 (0.04-40 nM) engages target gene expression in DMD patient muscle myoblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Chemical Information
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No. CAS 2095128-17-7
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Appearance Solid
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Peso molecular 476.49
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Fòrmula C25H27F3N2O4
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Color White to off-white
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SMILES
O=C(C[C@@H](CCCOC1=CC=CC=C1CN2C(C)=CN=C2C3=CC=C(C=C3)OC(F)(F)F)C)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : 43.33 mg/mL (90.94 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: 2.17 mg/mL (4.55 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.17 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 (21.7 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.
Pureza y Documentación
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Ficha de datos (277 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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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, 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 | 2.0987 mL | 10.4934 mL | 20.9868 mL | 52.4670 mL |
| 5 mM | 0.4197 mL | 2.0987 mL | 4.1974 mL | 10.4934 mL | |
| 10 mM | 0.2099 mL | 1.0493 mL | 2.0987 mL | 5.2467 mL | |
| 15 mM | 0.1399 mL | 0.6996 mL | 1.3991 mL | 3.4978 mL | |
| 20 mM | 0.1049 mL | 0.5247 mL | 1.0493 mL | 2.6233 mL | |
| 25 mM | 0.0839 mL | 0.4197 mL | 0.8395 mL | 2.0987 mL | |
| 30 mM | 0.0700 mL | 0.3498 mL | 0.6996 mL | 1.7489 mL | |
| 40 mM | 0.0525 mL | 0.2623 mL | 0.5247 mL | 1.3117 mL | |
| 50 mM | 0.0420 mL | 0.2099 mL | 0.4197 mL | 1.0493 mL | |
| 60 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8744 mL | |
| 80 mM | 0.0262 mL | 0.1312 mL | 0.2623 mL | 0.6558 mL |
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