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BMS-986166

Product NameBMS-986166
CAS1883345-06-9
MFC25H33NO2
MW379.54
EINECS
MOL File1883345-06-9.mol

Chemical Properties

Boiling point	543.0±50.0 °C(Predicted)
Density	1.095±0.06 g/cm3(Predicted)
pka	15.05±0.10(Predicted)

Usage And Synthesis

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

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