| Identification | Back Directory | [Name]
BMS-986166 | [CAS]
1883345-06-9 | [Synonyms]
BMS-986166
Udifitimod
((1R,3S)-1-amino-3-((S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol
Cyclopentanemethanol, 1-amino-3-[(6S)-5,6,7,8-tetrahydro-6-[2-(2-methoxyphenyl)ethyl]-2-naphthalenyl]-, (1R,3S)- | [Molecular Formula]
C25H33NO2 | [MOL File]
1883345-06-9.mol | [Molecular Weight]
379.54 |
| Hazard Information | Back Directory | [Uses]
Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases[1][2]. | [in vivo]
Udifitimod (0.1, 0.5 mg/kg; p.o.; once daily for 21 days) shows anti-inflammation activity in autoimmune encephalomyelitis model [1].
Udifitimod (0.1, 0.5 mg/kg; p.o.; once daily for 50 days) reduces the clinical score as well as the paw histology score in the collagen-induced arthritis (CIA) model[1]. | Animal Model: | 6-8 weeks, C57BL/6 female mice (autoimmune encephalomyelitis model (EAE))[2] | | Dosage: | 0.1, 0.5 mg/kg | | Administration: | P.o.; once daily for 21 days | | Result: | Showed a dose-dependent reduction in clinical scores for inflammation. |
| Animal Model: | DBA/1 mice (collagen-induced arthritis (CIA) model)[2] | | Dosage: | 0.1, 0.5 mg/kg | | Administration: | P.o.; once daily for 50 days | | Result: | Dose dependently reduced both the clinical score as well as the paw histology score following the dosing regimens. |
| [IC 50]
S1PR1 | [References]
[1] Bihorel S, et al. Population Pharmacokinetic Analysis of BMS-986166, a Novel Selective Sphingosine-1-Phosphate-1 Receptor Modulator, and Exposure-Response Assessment of Lymphocyte Counts and Heart Rate in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Jan;10(1):8-21. DOI:10.1002/cpdd.878
[2] Gilmore JL, et al. Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials. J Med Chem. 2019 Mar 14;62(5):2265-2285. DOI:10.1021/acs.jmedchem.8b01695 |
|
|