BMS-986251

• 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].

• UNSPSC :

  12352005

• Target :

  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 Formula :

  C30H29F8NO5S

• 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

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  IL-17; RORα; RORβ; RORγ

• CAS Number :

  [2460133-35-9]