GNE-3500

• Target:

  Others|||ROR

• Related Pathways:

  Others|||Metabolism

• Bioactivity:

  GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or ROR?) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, ROR?, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL) -17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 possessed favorable RORc cellular potency with 75-fold selectivity for RORc over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors in a cell assay panel. The favorable potency, selectivity, in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in a PK/PD model support the evaluation of GNE3500 in preclinical studies (J. Med. Chem., 2015, 58 (13), pp 5308–5322)

• Smiles:

  C[C@H]1CC[C@H](c2ccccc2)S(=O)(=O)N1Cc1ccc(cc1F)N1CCN(CC1)C(C)=O

• Molecular Formula:

  C24H30FN3O3S

• Molecular Weight:

  459.58

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  1537859-24-7