Glucocorticoid receptor agonist
Based on 1 publication(s) in Google Scholar
Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.
For research use only. We do not sell to patients.
- Purity: 98.34%
- CAS No.: 1245526-82-2
- Formula: C20H20F4N2O2
- Molecular Weight:396.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Glucocorticoid receptor agonist
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
80 nM
Compound: (R)-16
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Transactivation activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter by luciferase assay
Transactivation activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter by luciferase assay
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[PMID: 20735001] |
Glucocorticoid receptor agonist ((R)-16) has effect on IL-6 and MMTV with the IC50 values of 3.3 and 80 nM, respectively, also has effect on aromatase with the EC50 value of 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Glucocorticoid receptor agonist ((R)-16) (30 and 10 mg/kg, p.o., daily, 5 weeks) can reduce the increased levels of body fat and serum insulin and shows an effective inhibition of TNF-α production in LPS-stimulated mouse model[1].
The pharmacokinetic parameters of Glucocorticoid receptor agonist ((R)-16) in Sprague-Dawley rat (5 mg/kg i.v. or 30 mg/kg p.o.)[1].
| Parameters | Cl (i.v.)(mL/min/kg) | VSS(iv) (L/kg) | T1/2(iv)(h) | Cmax(po) (ng/mL) | AUCinf(po) (h·ng/mL) | F(po)% |
| (R)-16 | 49 | 7.6 | 1.85 | 509 | 4879 | 48 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1245526-82-2
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Appearance Solid
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Molecular Weight 396.38
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Formula C20H20F4N2O2
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Color White to yellow
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SMILES
OC1=CC=C(C=C1C(C)(C[C@](O)(C(F)(F)F)CC2=CC3=C(C=NC=C3)N2)C)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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : ≥ 100 mg/mL (252.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (6.31 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.31 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 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.
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.
Protocol
Animal administration [1] Female Balb/c mice weighing approximately 20 g were used. Mice were administered the test compound and in Cremophor (po) approximately 60 min prior to LPS/D-gal administration. The volume of oral gavage was 0.15 mL. Then mice were administered LPS (E. coli LPS 055:85, 1.0 μg/mouse) plus D-gal (50 mg/kg) intravenously in 0.2 mL of pyrogen-free saline. One hour after LPS/D-gal, each mouse was anesthetized, bled by cardiac puncture, and collected for serum TNF-R and compound levels. Blood samples were centrifuged at 2500 rpm for 10-15 min, the serum was decanted, and samples were stored frozen at -70°C until transfer either for TNF-R determination or to Drug Metabolism and Pharmacokinetics for plasma concentration analysis by HPLC. The concentration of TNF-R in the serum was measured by a commercially available ELISA kit. ELISA was performed. All samples are assayed in duplicate.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
References
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 | 2.5228 mL | 12.6142 mL | 25.2283 mL | 63.0708 mL |
| 5 mM | 0.5046 mL | 2.5228 mL | 5.0457 mL | 12.6142 mL | |
| 10 mM | 0.2523 mL | 1.2614 mL | 2.5228 mL | 6.3071 mL | |
| 15 mM | 0.1682 mL | 0.8409 mL | 1.6819 mL | 4.2047 mL | |
| 20 mM | 0.1261 mL | 0.6307 mL | 1.2614 mL | 3.1535 mL | |
| 25 mM | 0.1009 mL | 0.5046 mL | 1.0091 mL | 2.5228 mL | |
| 30 mM | 0.0841 mL | 0.4205 mL | 0.8409 mL | 2.1024 mL | |
| 40 mM | 0.0631 mL | 0.3154 mL | 0.6307 mL | 1.5768 mL | |
| 50 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2614 mL | |
| 60 mM | 0.0420 mL | 0.2102 mL | 0.4205 mL | 1.0512 mL | |
| 80 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7884 mL | |
| 100 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6307 mL |
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