SR 1555 (hydrochloride) |
| Catalog No.GC14418 |
inverse agonist of RORγ
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2309312-90-9
Sample solution is provided at 25 µL, 10mM.
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SR 1555 is a novel RORγ-specific synthetic ligand [1].
Retinoic acid receptor-related nuclear receptor (ROR) belongs to the nuclear receptor superfamily, a group of structurally related, ligand-dependent transcription factors. RORs function as key regulators of many physiological processes that occur during embryonic development and in the adult [2]. RORγ plays a dominant role in T cell differentiation, particularly in the development of TH17 cells, which are implicated in autoimmune diseases such as multiple sclerosis and rheumatoid arthritis [3].
In vitro: In a GAL4-NR chimeric co-transfection assay, SR1555 was devoid of LXR, FXR, and RORα activity, but it dose-dependently repressed the activity at RORγ with an IC50 of ≈ 1.5 μM. In competitive radioligand binding assays, SR1555 bound to RORγ with an IC50 of 1 μM. SR1555 specifically targeted RORγ and inhibited its transcriptional activity leading to suppression of IL-17 gene expression. EL4 cells treated SR1555 (10 μM) for 24 h inhibited Il17a gene expression by greater than 70%, demonstrating that SR1555 could inhibit the expression of this TH17 mediated cytokine [1]. SR1555 not only inhibited TH17 cell development and function but also increased the frequency of T regulatory cells [1].
References:
[1] Solt L A, Kumar N, He Y, et al. Identification of a selective RORγ ligand that suppresses Th17 cells and stimulates T regulatory cells[J]. ACS chemical biology, 2012, 7(9): 1515-1519.
[2] Jetten A M, Ueda E. The ROR nuclear orphan receptor subfamily: critical regulators of multiple biological processes[J]. Progress in nucleic acid research and molecular biology, 2001, 69: 205-247.
[3] Ivanov I I, McKenzie B S, Zhou L, et al. The orphan nuclear receptor RORγt directs the differentiation program of proinflammatory IL-17+ T helper cells[J]. Cell, 2006, 126(6): 1121-1133.
| Cas No. | 2309312-90-9 | SDF | |
| Chemical Name | 1-(4-((4'-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-[1,1'-biphenyl]-4-yl)methyl)piperazin-1-yl)ethanone, monohydrochloride | ||
| Canonical SMILES | O=C(C)N(CC1)CCN1CC2=CC=C(C3=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C3)C=C2.Cl | ||
| Formula | C22H22F6N2O2 • HCl | M.Wt | 496.9 |
| Solubility | ≤1.6mg/ml in ethanol;3mg/ml in DMSO;5mg/ml in dimethyl formamide | 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. |
||
| 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 | 2.0125 mL | 10.0624 mL | 20.1248 mL |
| 5 mM | 402.5 μL | 2.0125 mL | 4.025 mL |
| 10 mM | 201.2 μL | 1.0062 mL | 2.0125 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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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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