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NIBR-0213

Chemical Structure : NIBR-0213

CAS No.: 1233332-14-3

NIBR-0213 (NIBR 0213, NIBR0213)

Catalog No.: PC-61179Not For Human Use, Lab Use Only.

NIBR-0213 is a potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

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Biological Activity

NIBR-0213 is a potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).
NIBR-0213 displays potent and comparable potency on human and rat S1P1 with IC50 of 2.0 and 2.3 nM in GTPγ35S assays, 3,000-fold selectivity against human S1P5.
NIBR-0213 inhibits FTY720-phosphate-induced S1P1 internalization at 1 uM, induces long-lasting reduction of peripheral blood lymphocyte counts, shows comparable therapeutic efficacy to Fingolimod in experimental autoimmune encephalomyelitis (EAE).

Physicochemical Properties

M.Wt 464.98
Formula C27H29ClN2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[[3'-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]-L-alanine

References

1. Quancard J, et al. Chem Biol. 2012 Sep 21;19(9):1142-51.

2. Bigaud M, et al. PLoS One. 2016 Dec 22;11(12):e0168252.

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