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SLF80821178 is an inhibitor of the sphingosine-1-phosphate transporter (SPNS2).1 It reduces sphingosine-1-phosphate (S1P) secretion in HeLa cells with an IC50 value of 51 nM. Oral administration of SLF80821178 (100 mg/kg) decreases the number of circulating lymphocytes in mice, without reducing plasma S1P concentration. It reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE) induced by MOG35-55 (Item No. 35644) when administered at doses of 10 and 30 mg/kg per day.2 Unlike the loss of Spns2 function in Spns2-/- mice, inhibition of Spns2 by SLF80821178 does not induce neurosensorial hearing defects.
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1. Discovery of potent, orally bioavailable sphingosine-
2. Assessment of Spinster homologue 2 (Spns2)-