GNE-3500 |CAS:1537859-24-7 Probechem Biochemicals

Chemical Structure : GNE-3500

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GNE-3500 (GNE3500;GNE 3500)

货号: PC-60453Not For Human Use, Lab Use Only.

GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays.

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生物&药学活性

GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays.
GNE-3500 displays 75-fold selectivity over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors.
GNE-3500 inhibits the production of all three IL-17 subtypes in murine CD4+ T cells with EC50 of 0.27-1.8 uM, also inhibits the production of IL-17AA and -AF by ILCs.
GNE-3500 shows in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in vivo.

物理化学性质&存储条件

分子量	459.58
分子式	C24H30FN3O3S
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	1-[4-[3-Fluoro-4-[[(3S,6R)-tetrahydro-3-methyl-1,1-dioxido-6-phenyl-2H-1,2-thiazin-2-yl]methyl]phenyl]-1-piperazinyl]ethanone

参考文献

1. Fauber BP, et al. J Med Chem. 2015 Jul 9;58(13):5308-22.

GNE-3500 (GNE3500;GNE 3500)

生物&药学活性

物理化学性质&存储条件

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GNE-3500 (GNE3500;GNE 3500)

生物&药学活性

物理化学性质&存储条件

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