| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89627-5mg买3赠1 |
99.50% | ￥250.00 |
4 | - | - | - | - |
|
S89627-10mg买3赠1 |
99.50% | ￥370.00 |
5 | - | - | - | - |
|
S89627-25mg买3赠1 |
99.50% | ￥780.00 |
5 | - | - | - | - |
|
S89627-100mg促销 |
99.50% | ￥1860.00 ￥1480.00 |
3 | - | - | - | - |
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| 产品描述： | Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect | ||||||||||||||||||||
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| 靶点： | Phosphatase | ||||||||||||||||||||
| 体外研究： | Icerguastat (5 μM) 在应激条件下延长少突胶质细胞中的 eIF2α 磷酸化。 Icerguastat (Sephin1) (一种全磷酸酶的选择性抑制剂)，在体内安全和选择性地抑制蛋白磷酸酶 1 的调节亚基。Icerguastat 选择性结合并抑制应激诱导的 PPP1R15A，但不结合和抑制相关的组成型 PPP1R15B，以延长适应性磷酸信号通路的益处，保护细胞免受其他致命的蛋白质错误折叠应激 | ||||||||||||||||||||
| 体内研究： | Icerguastat (4-8 mg/kg；腹腔注射；每日一次，持续 35 天) 可延缓 EAE (实验性自身免疫性脑脊髓炎) 的发作。 Icerguastat (100 μg；ip) 延长了感染朊病毒的小鼠的存活时间。 Animal Model: C57BL/6J female mice immunized with MOG35-55/CFA to induce chronic EAE Dosage: 4 mg/kg, 8 mg/kg Administration: I.p.; daily for 35 days Result: Significantly delayed clinical disease onset with both dosages, but to a greater extent with the 8 mg/kg treatment. Animal Model: Five-week-old female FVB mice (intracerebrally with mouse-adapted RML prions) Dosage: 100 μg Administration: I.p.; 3 times per week for 60 days, after 60 days of treatment, the treatment was reduced to two i.p. injections per week for another 20 days. Result: Significantly prolonged survival of prion-infected mice. | ||||||||||||||||||||
| 参考文献： | 1. Chen Y, et al. Sephin1, which prolongs the integrated stress response, is a promising therapeutic for multiple sclerosis. Brain. 2019;142(2):344-361. 2. Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242 3. Thapa S, et al. Sephin1 Reduces Prion Infection in Prion-Infected Cells and Animal Model. Mol Neurobiol. 2020;57(5):2206-2219. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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