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GSK2981278

CAS No. : 1474110-21-8

MCE 站：GSK2981278

产品活性：GSK2981278 是一种有效的，选择性的 RORγ 反向激动剂。 GSK2981278 可以抑制 il17 启动子的激活并干扰 RORγ-DNA 结合。

研究领域：Metabolic Enzyme/Protease

作用靶点：ROR

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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