化合物Sinbaglustat T40542

Product Introduction
Bioactivity


英文名: Sinbaglustat

描述: Sinbaglustat (OGT2378) (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 可用于治疗溶酶体贮积症和研究溶酶体功能障碍相关的中枢神经退行性疾病。

体外活性: Sinbaglustat (OGT2378) (20 μM) leads to a remarkable reduction in the synthesis of glucosylceramide by 93% and ganglioside by >95% when compared to untreated MEB4 cells. This reduction occurs without inducing any cytotoxicity or antiproliferative effects.[1] Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS.[2]

体内活性: Sinbaglustat (OGT2378) (2500 mg/kg/day; p.o.; in the powdered chow; corresponding to 35-40 mg/mouse/day of Sinbaglustat; Female syngeneic C57BL/6 mice and bearing MEB4 melanoma tumor, 6-8 weeks old bearing MEB4 melanoma tumor) 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 46.66 mg/mL (200 mM)


关键字: OGT 2378 | ACT519276 | OGT-2378 | ACT 519276

相关产品: Tipifarnib (S enantiomer) | G43 | Alendronate sodium hydrate | Risedronate Sodium | 3-O-Methyltolcapone | Tipifarnib | (E)-Daporinad | Tolcapone | Tectol | Lonafarnib

相关库: Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途