SR 2211 |
| Catalog No.GC14284 |
inverse agonist of RORγ, potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1359164-11-6
Sample solution is provided at 25 µL, 10mM.
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SR 2211 is a potent and selective inverse agonist of RORγ with IC50 value of 320 nM [1].
RAR-related orphan receptor gamma (RORγ) is a nuclear receptor and a DNA-binding transcription factor. RORγ plays an important role in the regulation of circadian rhythms and Th17 cell differentiation [2].
SR 2211 is a potent and selective RORγ inverse agonist. SR2211 bound to RORγ with Ki value of 105 nM. SR2211 (10 μM) inhibited RORγ activity by 90% but didn’t affect the transcriptional activity of RORα and farnesoid X receptors (FXR). SR2211 showed weak activation of liver X receptor α (LXRα). In EL-4 murine T lymphocyte cell line, SR2211 (5 μM) followed by PMA/ionomycin significantly inhibited the expression of IL-17 and IL-23 receptor in a dose-dependent way [1]. Enriched naive CD4+ T cells under Th17 polarizing conditions, SR2211 significantly inhibited the production of IL-17, which suggested that SR2211 inhibited Th17 cell differentiation. In LPS-stimulated RAW 264.7 cells, SR2211 (5 μM) inhibited the expression of TNFα, IL-1β and IL-6, the proinflammatory cytokines that played an important role in the pathogenesis of RA [2].
Of the CIA mouse model, SR2211 (20 mg/kg) inhibited the development of arthritis in a dose-dependent way [2].
References:
[1]. Kumar N, Lyda B, Chang MR, et al. Identification of SR2211: a potent synthetic RORγ-selective modulator. ACS Chem Biol, 2012, 7(4): 672-677.
[2]. Chang MR, Lyda B, Kamenecka TM, et al. Pharmacologic Repression of Retinoic Acid Receptor-Related Orphan Nuclear Receptor γ Is Therapeutic in the Collagen-Induced Arthritis Experimental Model. Arthritis Rheumatol, 2014, 66(3): 579-588.
| Cas No. | 1359164-11-6 | SDF | |
| Chemical Name | 1,1,1,3,3,3-hexafluoro-2-(2-fluoro-4'-((4-(pyridin-4-ylmethyl)piperazin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)propan-2-ol | ||
| Canonical SMILES | FC1=CC(C(C(F)(F)F)(C(F)(F)F)O)=CC=C1C2=CC=C(C=C2)CN3CCN(CC4=CC=NC=C4)CC3 | ||
| Formula | C26H24F7N3O | M.Wt | 527.48 |
| Solubility | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8958 mL | 9.479 mL | 18.9581 mL |
| 5 mM | 0.3792 mL | 1.8958 mL | 3.7916 mL |
| 10 mM | 0.1896 mL | 0.9479 mL | 1.8958 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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