GSK 2981278

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK 2981278 (GSK2981278) 是一种有效的、高选择性的 RORγ/RORγt 抑制剂，可有效抑制人外周 T 细胞中 IL-17A 和 IL-22 蛋白的分泌，IC50 为 3.2 nM。

GSK 2981278 (GSK2981278) is a potent, highly selective RORγ/RORγt inhibitor that potently inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with IC50 of 3.2 nM; shows no effects on RORα-dependent activation; robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level, inhibits RORγt-mediated transactivation; attenuates inflammation in mouse model of psoriasis.Psoriasis Phase 2 Clinical(In Vitro):GSK2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions.GSK2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK2981278 led to a near-complete inhibition of IL-17A protein secretion.(In Vivo):GSK2981278 (1% in ointment; topically; for three days) reduces skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness. GSK2981278 attenuates inflammation in a mouse model of psoriasis.

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Animal Model:BALB/c JByRj Female Mice (8 week-old at study initiation; imiquimod (IMQ) mouse model) Dosage:1% Administration:In ointment; topically; for three days Result:Reduced skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness.

GSK2981278 | GSK-2981278

Nuclear Receptor/Transcription Factor

ROR

RORγ

Inflammation/Immunology

Psoriasis

1474110-21-8

461.617

C25H35NO5S

>98% (HPLC)

DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=S(C1=CC=C(OCC2CCOCC2)C(CO)=C1)(N(C3=CC=C(CC)C=C3)CC(C)C)=O

N-(4-Ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years