NIBR-0213

NIBR-0213

Stock Code: 3575818
Manufacturer Part No: SML2099-25MG
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£612.86 (exc VAT) per 25MG
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Application


NIBR-0213 may be used as a selective sphingosine-1-phosphate receptor 1 (S1P1) antagonist to assess S1P-mediated nuclear factor kappa B (NF-?B)-p65 nuclear translocation in human induced astrocytes.


Biochem/physiol Actions


NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist that blocks S1P1-selective ligand AUY954-induced Ca2+ mobilization (IC50 = 2.5 nM using human S1P1-transfected HeLa cells; IC50 >10 µM with human S1P2, S1P3, or S1P4 transfectants) and S1P-induced GTPγS recruitment (IC50 = 2.0/2.3/8.5 nM using membrane from human/murine/rat S1P1-transfected CHO cells; IC50 >10 µM with membrane from human S1P5 transfectant). NIBR-0213 induces long-lasting peripheral blood lymphocyte reduction in rats (EDmax = 1 mg/kg, ED50 = 0.2 mg/kg; p.o.) and exhibits therapeutic efficacy (30 mg/kg p.o; BID) in experimental autoimmune encephalomyelitis (EAE), a murine model of multiple sclerosis (MS), with no adverse effects to the animals.

Colourwhite to beige
ManufacturerSIGMA-ALDRICH
Storage Temp.−20°C
SolubilityDMSO: 2 mg/mL, clear
Formpowder
Assay≥98% (HPLC)

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