RORγt agonist 8-074

Chemical Structure : RORγt agonist 8-074

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货号: PC-49473Not For Human Use, Lab Use Only.

RORγt agonist 8-074 is a potent, selective RORγt agonist with Kd of 497 nM, shows potent RORγt agonist activity in the Gal4 reporter gene assay with EC50 of 118.7 nM, and EC50 of 19.95 nM in FRET assays.

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250 mg		Get quote

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生物&药学活性

RORγt agonist 8-074 is a potent, selective RORγt agonist with Kd of 497 nM, shows potent RORγt agonist activity in the Gal4 reporter gene assay with EC50 of 118.7 nM, and EC50 of 19.95 nM in FRET assays.
RORγt agonist 8-074 displayed high selectivity versus the other two ROR members.
RORγt agonist 8-074 demonstrates stimulating the mouse Tc17 cells with EC50 at 11.21 nM.
RORγt agonist 8-074 demonstrated potent and selective binding to the RORγt protein as well as potent in vitro activity compared with LYC-55716.
RORγt agonist 8-074 promoted the secretion of IL-17A by Th17 cells with EC50 of 22.78 nM.
RORγt agonist 8-074 (160 nM) significantly increased the percentage of CD4+ T and CD8+ T cells that express IL-17A (from 12.1% to 24.0% in CD4+ T and 22.9% to 50.4% in CD8+ T cells).
RORγt agonist 8-074 (50 mg/kg, i.p. injection, QD over two weeks) showed robust antitumor efficacy in syngeneic tumor models, and 8-074 improved the efficacy of anti‑PD‑1 therapy in murine lung cancer models.

物理化学性质&存储条件

分子量	528.590
分子式	C28H27F3N2O3S
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-(3'-cyano-4'-isobutyl-2-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide

参考文献

1. Li Xia, et al. J Exp Clin Cancer Res. 2022 Apr 23;41(1):155.