SR 2211inverse agonist of RORγ, potent and selective CAS# 1359164-11-6 |
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Quality Control & MSDS
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| Cas No. | 1359164-11-6 | SDF | Download SDF |
| PubChem ID | 51035449 | Appearance | Powder |
| Formula | C26H24F7N3O | M.Wt | 527.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 50 mM in 1eq. HCl | ||
| Chemical Name | 1,1,1,3,3,3-hexafluoro-2-[3-fluoro-4-[4-[[4-(pyridin-4-ylmethyl)piperazin-1-yl]methyl]phenyl]phenyl]propan-2-ol | ||
| SMILES | C1CN(CCN1CC2=CC=C(C=C2)C3=C(C=C(C=C3)C(C(F)(F)F)(C(F)(F)F)O)F)CC4=CC=NC=C4 | ||
| Standard InChIKey | KVHKWAZUPPBMLL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C26H24F7N3O/c27-23-15-21(24(37,25(28,29)30)26(31,32)33)5-6-22(23)20-3-1-18(2-4-20)16-35-11-13-36(14-12-35)17-19-7-9-34-10-8-19/h1-10,15,37H,11-14,16-17H2 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective inverse agonist of retinoic acid receptor-related orphan receptor γ (RORγ) (Ki = 105 nM; IC50 ~320 nM). Exhibits weak activity at liver X receptor α (LXRα); does not affect the transcriptional activity of farnesoid X receptors (FXR), and has no impact on the transcriptional activity of RORα. |
SR 2211 Dilution Calculator
SR 2211 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8958 mL | 9.479 mL | 18.9581 mL | 37.9161 mL | 47.3952 mL |
| 5 mM | 0.3792 mL | 1.8958 mL | 3.7916 mL | 7.5832 mL | 9.479 mL |
| 10 mM | 0.1896 mL | 0.9479 mL | 1.8958 mL | 3.7916 mL | 4.7395 mL |
| 50 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.7583 mL | 0.9479 mL |
| 100 mM | 0.019 mL | 0.0948 mL | 0.1896 mL | 0.3792 mL | 0.474 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Identification of SR2211: a potent synthetic RORgamma-selective modulator.[Pubmed:22292739]
ACS Chem Biol. 2012 Apr 20;7(4):672-7.
Nuclear receptors (NRs) are ligand-regulated transcription factors that display canonical domain structure with highly conserved DNA-binding and ligand-binding domains. The identification of the endogenous ligands for several receptors remains elusive or is controversial, and thus these receptors are classified as orphans. One such orphan receptor is the retinoic acid receptor-related orphan receptor gamma (RORgamma). An isoform of RORgamma, RORgammat, has been shown to be essential for the expression of Interleukin 17 (IL-17) and the differentiation of Th17 cells. Th17 cells have been implicated in the pathology of several autoimmune diseases, including multiple sclerosis (MS) and rheumatoid arthritis (RA). Genetic ablation of RORgamma alone or in combination with RORalpha in mice led to impaired Th17 differentiation and protected the mice from development of experimental autoimmune encephalomyelitis (EAE), a mouse model of MS. Here we describe SR2211, a selective RORgamma modulator that potently inhibits production of IL-17 in cells.
