NIBR-0213

NIBR-0213

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.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575818 NIBR-0213 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£612.86 (exc VAT) per 25MG
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3575819 NIBR-0213 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£136.50 (exc VAT) per 5MG
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