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2460133-35-9

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2460133-35-9 Structure

2460133-35-9 Structure
IdentificationBack Directory
[Name]

Cyclohexanecarboxylic acid, 4-[[(3aR,9bR)-9b-[(4-fluorophenyl)sulfonyl]-1,2,3a,4,5,9b-hexahydro-7-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]-3H-benz[e]indol-3-yl]carbonyl]-3-methyl-, (1R,3S,4R)-
[CAS]

2460133-35-9
[Synonyms]

BMS-986251
Cyclohexanecarboxylic acid, 4-[[(3aR,9bR)-9b-[(4-fluorophenyl)sulfonyl]-1,2,3a,4,5,9b-hexahydro-7-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]-3H-benz[e]indol-3-yl]carbonyl]-3-methyl-, (1R,3S,4R)-
[Molecular Formula]

C30H29F8NO5S
[MOL File]

2460133-35-9.mol
[Molecular Weight]

667.61
Chemical PropertiesBack Directory
[Boiling point ]

691.5±55.0 °C(Predicted)
[density ]

1.444±0.06 g/cm3(Predicted)
[pka]

4.81±0.16(Predicted)
Hazard InformationBack Directory
[Uses]

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].
[in vivo]

BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness[1].
BMS-986251 (0.13, 0.79, 4.76 mg/kg; orally; once a day) displays a dose-dependent reduction of the IL-17F produced in na?ve C57BL/6 female mice (7-9 weeks)[1].
BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a Vss of 1.9 L/kg for IV in mouse[1].

Animal Model:C57BL/6 female mice with acanthosis[1]
Dosage:5, 15, 45 mg/kg
Administration:Orally; twice daily until day 9
Result:Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening.
Animal Model:Mouse or rat[1]
Dosage:2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis)
Administration:IV or PO
Result:Had a T1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a Vss of 1.9 L/kg for IV in mouse.
Had a Cmax of 4.8 μM and an AUC of 37 μM?h for PO in mouse.
Had a T1/2 of 11 hours, a CL of 1.3 mL/min?kg, and a Vss of 1.25 L/kg for IV in rat.
Had a Cmax of 4.7 μM and an AUC of 64 μM?h for PO in rat.
[IC 50]

RORγt: 12 nM (EC50); IL-17: 24 nM (EC50); RORα: >10 μM (EC50); RORβ: >10 μM (EC50)
[References]

[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 DOI:10.1021/acsmedchemlett.0c00063
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