NIBR189

NIBR189

Biochem/physiol Actions

NBIR189 is a high-affinity, potent and selective EBI2 (GPR183) antagonist (IC50 = 16 nM against 10 nM 7A,25-OHC for binding human EBI2) that inhibits 7A,25-OHC-induced GTPγS binding (IC50 = 8.5 and 7.0 nM, respectively, against 0.33 and 0.1 nM OHC; human EBI2-expressing CHO membrane), calcium mobilization (IC50 = 11 and 15 nM using human or mouse EBI2-transfected cells, respectively), and chemotaxis (IC50 = 0.3 nM against 20 nM OHC-induced U937 migration). NBIR189 displays no inhibitory potency against 5HT2A, muscarinic acetylcholine receptor M2, adrenoreceptor A1A, nor significant affintiy toward 18 other GPCRs/transporters/enzymes, and exhibits good pharmacokinetic properties and oral availability in mice (AUC = 3608 nmol h/L, Cmax = 835 nM, tmax = 1 h, F = 49%; 3 mg/kg p.o.). A useful tool for probing EBI2-mediated physiological functions and autoimmune disorders.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575654 NIBR189 white to beige SIGMA-ALDRICH room temp DMSO: 10 mg/mL, clear (warmed) powder ≥98% (HPLC)
£490.29 (exc VAT) per 25MG
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3575655 NIBR189 white to beige SIGMA-ALDRICH room temp DMSO: 10 mg/mL, clear (warmed) powder ≥98% (HPLC)
£142.07 (exc VAT) per 5MG
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