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Beschreibung

A highly potent and specific oxysterol EBI2 (GPR183) agonist with a kd of 450 pM in a saturation binding analysis, and activates EBI2 (EC50=140 pM compared with 2.1nM for its enantiomer 7b,25-OHC) in a GTP-gamma assay. Dose-dependenty suppresses forskolin-induced cAMP accumulation in EBI2-expressing SK-N-MC/CRE-beta galactosidase cell line with an IC50 of 2 nM, but not in control cells. Stimulates migration of LPS-activated spleen B cells and T cells in a dose-dependent manner. In addition, pharmacological inhibition of its biosynthesis in vivo by Clotrimazole, a CYP7B1inhibitor promotes the migration of adoptively transferred pre-activated B cells to the T/B boundary, mimicking the phenotype of pre-activated B cells from EBI2-deficient mice.

Strukturformel

SAF-128136-1MG

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