GSK2981278 |
| Catalog No.GC13905 |
RORγ-selective inverse agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1474110-21-8
Sample solution is provided at 25 µL, 10mM.
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GSK2981278 is a RORγ-selective inverse agonist.
RAR-related orphan receptor gamma (RORγ) is a protein that in humans is encoded by the RORC gene. The RORγ protein is a DNA-binding transcription factor and is a member of the NR1 subfamily of nuclear receptors.
In vitro: Previous study found that GSK2981278 had no significant effect on RORα-dependent activation, indicating its selectivity for RORγ. GSK2981278 also demonstrated 10-fold greater potency for IL-17A inhibition than its analogs of GSK3038548 and GSK3038549. In addition, authors examined the effect of GSK2981278 on endogenous il17a expression in Jurkat cells. Results showed that GSK2981278 could repress the activation of il17a by RORγt in a dose-responsive manner [1].
In vivo: In previous study, the imiquimod (IMQ) mouse model was employed to demonstrate efficacy of GSK2981278 in a psoriaform-like mouse model. Results showed that the topical application of IMQ could induce and exacerbate psoriasis-like chronic skin inflammation in mice. Next, mice were treated topically with GSK2981278 for three days, after which mice continued to receive compound for the duration of the study. It was found that GSK2981278 was undetectable in serum at harvest, suggesting that systemic exposure was minimal. In addition, mice exposed to GSK2981278 exhibited reduced skin redness and scaling, as well as decreased hyperplasia [1].
Clinical trial: The study of safety and efficacy of topical GSK2981278 ointment in plaque psoriasis has been finished but there is no results released [2].
References:
[1] Smith SH et al. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.
[2] https://clinicaltrials. gov/ct2/show/NCT02548052 term=GSK2981278&rank=2
| Cas No. | 1474110-21-8 | SDF | |
| Chemical Name | N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide | ||
| Canonical SMILES | OCC1=CC(S(N(CC(C)C)C2=CC=C(CC)C=C2)(=O)=O)=CC=C1OCC3CCOCC3 | ||
| Formula | C25H35NO5S | M.Wt | 461.6 |
| Solubility | ≤15mg/ml in ethanol;5mg/ml in DMSO;30mg/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. |
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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 | 2.1664 mL | 10.8319 mL | 21.6638 mL |
| 5 mM | 0.4333 mL | 2.1664 mL | 4.3328 mL |
| 10 mM | 0.2166 mL | 1.0832 mL | 2.1664 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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