1537859-24-7

1537859-24-7 structure

Name: GNE-3500
Chemical Name: 1-[4-(3-Fluoro-4-{[(3S,6R)-3-methyl-1,1-dioxido-6-phenyl-1,2-thiazinan-2-yl]methyl}phenyl)-1-piperazinyl]ethanone
CAS Number: 1537859-24-7
Molecular Formula: C₂₄H₃₀FN₃O₃S
Molecular Weight: 459.577
Create Date: 2020-01-11 17:35:49
Modify Date: 2024-02-29 12:59:50
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.

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

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