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描述 | GSK2981278 is recognized as a potent and selective inverse agonist of RORγ, effectively inhibiting the activation of the IL17 promoter and disrupting RORγ-DNA binding[1]. |
体内研究 | Topical application of GSK2981278 (1% in ointment; for three days) results in a reduction of skin redness and scaling, along with a 23% reduction in epidermal thickness, indicating its effectiveness in attenuating inflammation in a mouse model of psoriasis[1]. |
体外研究 | GSK2981278 significantly suppresses IL-17A and IL-22 protein secretion in a concentration-dependent manner with an IC50 of 3.2 nM, especially noticeable during 5 days of culture under Th17 skewing conditions[1]. At varying concentrations (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; over 5 days), GSK2981278 shows potent and selective inhibition of IL-17 and IL-22 levels, with concentrations ≥3 nM leading to nearly complete inhibition of IL-17A protein secretion[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.66mL 4.33mL 2.17mL |
CAS号 | 1474110-21-8 |
分子式 | C25H35NO5S |
分子量 | 461.614 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(227.46 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |