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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-GSK2981278
GSK2981278

Chemical Structure : GSK2981278

CAS No.: 1474110-21-8

GSK2981278 (GSK-2981278)

货号: PC-60455Not For Human Use, Lab Use Only.

GSK2981278 (GSK-2981278) is a potent, highly selective RORγ antagonist that potently inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with IC50 of 3.2 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2981278 (GSK-2981278) is a potent, highly selective RORγ antagonist that potently inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with IC50 of 3.2 nM.
GSK2981278 shows no effects on RORα-dependent activation.
GSK2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level, inhibits RORγt-mediated transactivation; attenuates inflammation in mouse model of psoriasis.

物理化学性质&存储条件

分子量 461.617
分子式 C25H35NO5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Kang EG, et al. Br J Dermatol. 2017 Nov 18. doi: 10.1111/bjd.16131.

2. Smith SH, et al. PLoS One. 2016 Feb 12;11(2):e0147979.

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