Sinbaglustat

Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase ( GCS ) and non-lysosomal glucosyl ceramidase ( GBA2 ). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions. In Vitro Sinbaglustat (OGT2378; 20 μM) reduces the synthesis of glucosylceramide and ganglioside by 93% and >95% in MEB4 melanoma cells compared with untreated MEB4 cells, respectively, without either cytotoxic or antiproliferative effects. GBA2 is an enzyme involved in the catabolism of glycosphingolipids (GSLs). Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Sinbaglustat (OGT2378; administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day, corresponding to 35-40 mg of Sinbaglustat per mouse per day) is highly effective in impeding melanoma tumor growth in vivo. The effectiveness of p.o. Sinbaglustat in this murine model suggests that inhibition of glycosphingolipid synthesis is a promising approach to inhibit tumor progression . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor Dosage: 35-40 mg per mouse per day Administration: Administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day Result: Inhibited MEB4 melanoma tumor growth in a syngeneic, orthotopic murine model. Form:Solid

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