GSK805

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK805 是一种有效的、口服生物可利用的视黄醇相关孤儿受体 γ t (RORγt) 反向激动剂，可与受体的推定配体结合域相互作用，而不会对 DNA 结合产生显着影响。

GSK805 is a potent orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.

Cell Differentiation Assay Cell Line:CD4+ T cells Concentration:0.5 μM Incubation Time:4 days Result:Inhibited IL-17 production during Th17 cell differentiation.

GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE).GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice. Animal Model:C57BL/6 mice were immunized with MOG35–55 plus CFA Dosage:10 mg/kg Administration:Oral gavage; 10 mg/kg once per day; for 35 days Result:Efficiently ameliorated the severity of EAE in mice.Animal Model:C57BL/6 mice with EAE Dosage:30 mg/kg Administration:Oral gavage; 30 mg/kg once Result:Reduced both IFN-γ-IL-17+ and IFN-γ+IL-17+ T cells without altered the frequency of TNF-α+ T cells in EAE mice.

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Nuclear Receptor/Transcription Factor

ROR

RORγt

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1426802-50-7

532.36

C23H18Cl2F3NO4S

>98% (HPLC)

DMSO:100 mg/mL (187.84 mM)

CCS(=O)(=O)c1ccc(CC(=O)Nc2cc(Cl)c(c(Cl)c2)-c2ccccc2OC(F)(F)F)cc1

N-[26-dichloro-2'-(trifluoromethoxy)[11'-biphenyl]-4-yl]-4-(ethylsulfonyl)-benzeneacetamide

(-20℃)

With Ice Pack

≥ 2 years