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O-GlcNAcase-IN-2(化合物81)是一种具口服活性、能穿透血脑屏障的OGA抑制剂,其IC50值为4.93 nM。该化合物能显著增加蛋白质的O-GlcNAcylation水平,并在OA损伤的SH-SY5Y细胞模型中降低tau蛋白的磷酸化状态(p-Ser199、p-Thr205和p-Ser396)。此外,O-GlcNAcase-IN-2还能改善APP/PS1小鼠模型的认知功能,显示出其对抗阿兹海默症(AD)的潜力。
O-GlcNAcase-IN-2(化合物81)是一种具口服活性、能穿透血脑屏障的OGA抑制剂,其IC50值为4.93 nM。该化合物能显著增加蛋白质的O-GlcNAcylation水平,并在OA损伤的SH-SY5Y细胞模型中降低tau蛋白的磷酸化状态(p-Ser199、p-Thr205和p-Ser396)。此外,O-GlcNAcase-IN-2还能改善APP/PS1小鼠模型的认知功能,显示出其对抗阿兹海默症(AD)的潜力。
规格 | 价格 | 库存 | 数量 |
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10 mg | 询价 | 期货 | |
50 mg | 询价 | 期货 |
产品描述 | O-GlcNAcase-IN-2 (compound 81) is an orally active, brain-penetrant inhibitor of O-GlcNAcase, demonstrating an IC50 value of 4.93 nM. It has shown potential in elevating protein O-GlcNAcylation levels and promoting phosphorylation of tau (p-Ser199, p-Thr205, p-Ser396) in an OA-impacted SH-SY5Y cell model. Additionally, O-GlcNAcase-IN-2 has been observed to ameliorate cognitive deficits in APP/PS1 mice, suggesting its potential utility in combating Alzheimer's disease (AD). |
分子量 | 394.53 |
分子式 | C22H26N4OS |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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