BMS-986251

• UNSPSC Description:

  BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis)[1].

• Target Antigen:

  Interleukin Related; ROR

• Type:

  Reference compound

• Related Pathways:

  Immunology/Inflammation;Metabolic Enzyme/Protease;Vitamin D Related/Nuclear Receptor

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/bms-986251.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C([C@H]1C[C@H](C)[C@H](C(N2CC[C@@]3(S(=O)(C4=CC=C(F)C=C4)=O)C5=CC=C(C(C(F)(F)F)(F)C(F)(F)F)C=C5CC[C@@]23[H])=O)CC1)O

• Molecular Weight:

  667.61

• References & Citations:

  [1]Robert J. Cherney, et al. Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist. ACS Med. Chem. Lett. 2020, 11, 6, 1221–1227

• Shipping Conditions:

  Room temperature

• Clinical Information:

  Phase 2

• CAS Number:

  2460133-35-9