Sinbaglustat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sinbaglustat (OGT2378) 是葡萄糖神经酰胺合成酶 (GCS) 和非溶酶体葡萄糖神经酰胺酶 (GBA2) 的双重抑制剂。Sinbaglustat 是一种可透过血脑屏障的的口服N-烷基亚氨基糖。Sinbaglustat 可用于与溶酶体功能障碍相关的中枢神经退行性疾病的研究。

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.

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.

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.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.

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Metabolic Enzyme/Protease

Transferase

Transferase

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441061-33-2

233.3

C11H23NO4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (357.18 mM; 超声助溶 )

CCCCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@@H]1CO

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(-20℃)

With Ice Pack

≥ 2 years