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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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *