C108297
Based on 1 Customer Validation
C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 864972-30-5
- Formula: C30H36FN3O4S
- Molecular Weight:553.69
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Chemical Information
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CAS No. 864972-30-5
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Appearance Solid
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Molecular Weight 553.69
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Formula C30H36FN3O4S
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Color White to off-white
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SMILES
COCCOC[C@]12CC3=C(C=C1CCN(C2)S(=O)(C4=CC=C(C=C4)C(C)(C)C)=O)N(N=C3)C5=CC=C(C=C5)F
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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 (180.61 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 (4.52 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.
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]. Clark RD, et al. 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. Bioorg Med Chem Lett. 2008;18(4):1312-1317. [Content Brief]
[2]. van den Heuvel JK, et al. Identification of a selective glucocorticoid receptor modulator that prevents both diet-induced obesity and inflammation. Br J Pharmacol. 2016;173(11):1793-1804. [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 | 1.8061 mL | 9.0303 mL | 18.0606 mL | 45.1516 mL |
| 5 mM | 0.3612 mL | 1.8061 mL | 3.6121 mL | 9.0303 mL | |
| 10 mM | 0.1806 mL | 0.9030 mL | 1.8061 mL | 4.5152 mL | |
| 15 mM | 0.1204 mL | 0.6020 mL | 1.2040 mL | 3.0101 mL | |
| 20 mM | 0.0903 mL | 0.4515 mL | 0.9030 mL | 2.2576 mL | |
| 25 mM | 0.0722 mL | 0.3612 mL | 0.7224 mL | 1.8061 mL | |
| 30 mM | 0.0602 mL | 0.3010 mL | 0.6020 mL | 1.5051 mL | |
| 40 mM | 0.0452 mL | 0.2258 mL | 0.4515 mL | 1.1288 mL | |
| 50 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9030 mL | |
| 60 mM | 0.0301 mL | 0.1505 mL | 0.3010 mL | 0.7525 mL | |
| 80 mM | 0.0226 mL | 0.1129 mL | 0.2258 mL | 0.5644 mL | |
| 100 mM | 0.0181 mL | 0.0903 mL | 0.1806 mL | 0.4515 mL |