GSK2981278

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Chemical Information

Product name：GSK2981278	Purity：99% min
CAS NO：1474110-21-8	Solubility：DMSO : ≥ 100 mg/mL (216.63 mM)
Molecular Formula：C₂₅H₃₅NO₅S	Package：Package according to customer requirements
Molecular Weight：461.614	Storage：Store at -20℃

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Remarks

GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). GSK2981278 is a strong RORγ-selective inverse agonist that inhibits activation of the il17 promoter. GSK2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level. 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.

References

[1]. Birault Veronique, et al. Preparation of tetrahydropyranylmethoxy benzenesulfonamide compounds as RORγ modulators useful in therapy of various diseases. From PCT Int. Appl. (2015), WO 2015061515 A1 20150430.

[2]. Birault Veronique, et al. Preparation of tertiary N-arylbenzenesulfonamides as RORγ modulators useful in treatment of inflammatory, metabolic, and autoimmune diseases. From PCT Int. Appl. (2013), WO 2013160418 A1 20131031.