Glucocorticoid receptor modulator 1 |
| Catalog No.GC71181 |
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2868357-11-1
Sample solution is provided at 25 µL, 10mM.
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Glucocorticoid receptor modulator 1 (compound B53) shows inhibitory activities against NF-κB and AP-1 with IC50s of 9 nM and 130 nM, respectively[1].
Glucocorticoid receptor modulator 1 (10 μM; 24 h) decreases the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2[1].
Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; p.o.; for 24 days) relieves dermatitis in mice and suppresses the expression of inflammatory factors[1].
References:
[1]. Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18.
| Cas No. | 2868357-11-1 | SDF | |
| Formula | C24H23ClN2O4S | M.Wt | 470.97 |
| Solubility | DMSO : 100 mg/mL (212.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) | Storage | 4°C, sealed storage, away from moisture and light |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1233 mL | 10.6164 mL | 21.2328 mL |
| 5 mM | 0.4247 mL | 2.1233 mL | 4.2466 mL |
| 10 mM | 0.2123 mL | 1.0616 mL | 2.1233 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 ddH2O, 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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