产品描述
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.
体外活性
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[1]. GBA2 is an enzyme involved in the catabolism of glycosphingolipids (GSLs).?Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS[2].
体内活性
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[1]. Animal Model: Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor[1]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.
Cas No.
441061-33-2
分子式
C11H23NO4
分子量
233.3
别名
ACT-519276;OGT2378;Sinbaglustat;Sinbaglustat
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years