Glucocorticoid receptor agonist |
Catalog No.GC11399
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1245526-82-2
Sample solution is provided at 25 µL, 10mM.
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Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
Reference：
[1]. Riether, Doris et al.Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. Journal of Medicinal Chemistry (2010), 53(18), 6681-6698.
Animal experiment: | 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. |
References: [1]. Riether, Doris et al.Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. Journal of Medicinal Chemistry (2010), 53(18), 6681-6698. | |
| Cas No. | 1245526-82-2 | SDF | |
| Chemical Name | 4-fluoro-2-[(4R)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol | ||
| Canonical SMILES | CC(C)(CC(CC1=CC2=C(N1)C=NC=C2)(C(F)(F)F)O)C3=C(C=CC(=C3)F)O | ||
| Formula | C20H20F4N2O2 | M.Wt | 396.38 |
| Solubility | DMSO : ≥ 100 mg/mL (252.28 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5228 mL | 12.6142 mL | 25.2283 mL |
| 5 mM | 504.6 μL | 2.5228 mL | 5.0457 mL |
| 10 mM | 252.3 μL | 1.2614 mL | 2.5228 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)