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BMS-986251

CAT: 0804-HY-136527Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-136527Size:1 Each
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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 models (preclinical models of psoriasis).
CAS Number
2460133-35-9
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

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