GNE-3500

GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats[1].

Product Specifications

CAS Number

[1537859-24-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

ROR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gne-3500.html

Purity

98.90

Smiles

FC1=CC(N2CCN(C(C)=O)CC2)=CC=C1CN3[C@@H](C)CC[C@H](C4=CC=CC=C4)S3(=O)=O

Molecular Formula

C24H30FN3O3S

Molecular Weight

459.58

Precautions

H302, H315, H319, H335

References & Citations

[1]Fauber BP, et al., Discovery of 1-{4-[3-fluoro-4- ((3s,6r) -3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl) -phenyl]-piperazin-1-yl}-ethanone (GNE-3500) : a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist. J Med Chem. 2015 Jul 9;58 (13) :5308-22.