GNE-3500

Names

[ Name ]:
GNE-3500

[Synonym ]:
1-[4-(3-Fluoro-4-{[(3S,6R)-3-methyl-1,1-dioxido-6-phenyl-1,2-thiazinan-2-yl]methyl}phenyl)-1-piperazinyl]ethanone
Ethanone, 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]-

Biological Activity

[Description]:

GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays; displays 75-fold selectivity over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors; 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; shows in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in vivo.

[References]

References 1. Fauber BP, et al. J Med Chem. 2015 Jul 9;58(13):5308-22. View Related Products by Target ROR

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
664.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₃₀FN₃O₃S

[ Molecular Weight ]:
459.577

[ Flash Point ]:
355.6±34.3 °C

[ Exact Mass ]:
459.199188

[ LogP ]:
3.24

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.592

Related Compounds

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