BMS-986251 | RORγt inhibitor | Probechem Biochemicals

Chemical Structure : BMS-986251

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BMS-986251 (BMS 986251)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	667.611
分子式	C30H29F8NO5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1R,3S,4R)-4-((3aR,9bR)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)- 2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole-3-carbonyl)-3-methylcyclohexane-1-carboxylic acid

参考文献

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.

BMS-986251 (BMS 986251)

生物&药学活性

物理化学性质&存储条件

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BMS-986251 (BMS 986251)

生物&药学活性

物理化学性质&存储条件

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