GSK2981278

Catalog No.S6610

For research use only.

GSK2981278 is a highly potent and selective inverse agonist for RORγ.

GSK2981278 Chemical Structure

CAS No. 1474110-21-8

Purity & Quality Control

Choose Selective ROR Inhibitors

Biological Activity

Description GSK2981278 is a highly potent and selective inverse agonist for RORγ.
Targets
RORγ [1]
In vitro

GSK2981278 has no significant effect on RORα-dependent activation. GSK2981278 significantly inhibits production of the Th17 signature (IL-17A, IL-17F, IL-22 and IL-23) in multiple in vitro and human tissue-based assays[1].

In vivo

GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 will significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 461.61
Formula

C25H35NO5S

CAS No. 1474110-21-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=CC=C(C=C1)N(CC(C)C)S(=O)(=O)C2=CC(=C(C=C2)OCC3CCOCC3)CO

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03004846 Completed Drug: GSK2981278 ointment|Drug: Vehicle ointment Psoriasis GlaxoSmithKline February 13 2017 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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