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Chemical Structure| 1474110-21-8 Chemical Structure| 1474110-21-8

Structure of GSK2981278
CAS No.: 1474110-21-8

Chemical Structure| 1474110-21-8

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GSK2981278 is a retinoid-related orphan receptor gamma (RORy) modulator.

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Product Details of GSK2981278

CAS No. :1474110-21-8
Formula : C25H35NO5S
M.W : 461.61
SMILES Code : CC(C)CN(S(=O)(C1=CC=C(OCC2CCOCC2)C(CO)=C1)=O)C3=CC=C(CC)C=C3
MDL No. :MFCD29059455
InChI Key :LZLBRISQTJVZNP-UHFFFAOYSA-N
Pubchem ID :89875987

Safety of GSK2981278

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Description
GSK2981278 is recognized as a potent and selective inverse agonist of RORγ, effectively inhibiting the activation of the IL17 promoter and disrupting RORγ-DNA binding[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
bursal B lymphocyte 1 μM 30 min As a RORγ antagonist, GSK2981278 mimicked the inhibitory effect of melatonin on B-lymphocyte apoptosis, decreased IL-6, TNF-α, IFN-γ and ROS production, down-regulated p-iκb and p-p65 protein expression, whereas it improved the IL-10 level and Nrf2 and HO-1 protein expression. PMC9029876
bursal B lymphocytes 1 μM 30 min GSK2981278, as a RORγ antagonist, co-treated with LPS and melatonin, significantly reduced the expression of Bax and Caspase-3 proteins, increased the expression of Bcl-2 protein, and inhibited the apoptosis of B lymphocytes. PMC9029876

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.66mL

4.33mL

2.17mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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