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Chemical Structure : BMS-986251
Catalog No.: PC-38350Not For Human Use, Lab Use Only.
BMS-986251 is a potent, selective, orally active RORγt inverse agonist with EC50 of 12 nM in GAL-4 reporter assay in Jurkat cell line, and 24 nM in IL-17 human whole blood assay.
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BMS-986251 is a potent, selective, orally active RORγt inverse agonist with EC50 of 12 nM in GAL-4 reporter assay in Jurkat cell line, and 24 nM in IL-17 human whole blood assay.
BMS-986251 displays high selectivity over ROR family members (RORα and RORβ) and other nuclear receptors (PXR, LXRα, and LXRβ) with IC50 >5,000 nM.
BMS-986251 inhibits IL-17F production in IL-2/IL-23 stimulated mouse pharmacodynamic (PD) model.
BMS-986251 reduces ear thickness in mouse acanthosis model, 15 mg/kg dose of BMS-986251 is comparable to the human anti-IL-23.
| M.Wt | 667.611 | |
| Formula | C30H29F8NO5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Cherney RJ, et al. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227.
2. Haggerty HG, et al. Toxicol Sci. 2021 Aug 30;183(1):93-104.
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