货号	规格	价格	上海	北京	珠海	重庆	武汉
S83443-1mg买3赠1	99.20%	￥160.00 S83443-1mg ￥160.00 现货（买3赠1）	9 9	-	-	-	-
S83443-5mg买3赠1	99.20%	￥260.00 S83443-5mg ￥260.00 现货（买3赠1）	9 9	-	-	-	-
S83443-10mg买3赠1	99.20%	￥390.00 S83443-10mg ￥390.00 现货（买3赠1）	8 8	-	-	-	-
S83443-50mg促销	99.20%	￥620.00 ￥496.00 S83443-50mg ￥496.00 现货	6 6	-	-	-	-
S83443-100mg促销	≥99%	￥840.00 ￥672.00 S83443-100mg ￥672.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding

靶点：

RORγ;ROR

体外研究：

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

体内研究：

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. 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.

参考文献：

1. Smith SH, et al. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.166 ml	10.832 ml	21.663 ml
5 mM	0.433 ml	2.166 ml	4.333 ml
10 mM	0.217 ml	1.083 ml	2.166 ml
50 mM	0.043 ml	0.217 ml	0.433 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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