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Icerguastat (IFB-088) 是一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物,是一种磷酸酶调节亚单位 PPP1R15A (R15A)的选择性抑制剂。它能够抑制 eIF2α 去磷酸化,从而延长保护反应。它具有抗朊病毒作用。
Icerguastat (IFB-088) 是一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物,是一种磷酸酶调节亚单位 PPP1R15A (R15A)的选择性抑制剂。它能够抑制 eIF2α 去磷酸化,从而延长保护反应。它具有抗朊病毒作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 118 | 现货 | |
5 mg | ¥ 271 | 现货 | |
10 mg | ¥ 398 | 现货 | |
25 mg | ¥ 833 | 现货 | |
50 mg | ¥ 1,290 | 现货 | |
100 mg | ¥ 1,990 | 现货 | |
200 mg | ¥ 2,750 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 233 | 现货 |
产品描述 | Icerguastat (IFB-088) is a selective inhibitor of holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo. |
体外活性 | Sephin1 dose and time dependently reduced PrPSc in different neuronal cell lines which were persistently infected with various prion strains. In addition, prion seeding activity was reduced in Sephin1-treated cells. Importantly, we found that Sephin1 significantly overcame the endoplasmic reticulum (ER) stress induced in treated cells, as measured by lower expression of stress-induced aberrant prion protein[1]. |
体内活性 | In a mouse model of prion infection, intraperitoneal treatment with Sephin1 significantly prolonged survival of prion-infected mice. When combining Sephin1 with the neuroprotective drug metformin, the survival of prion-infected mice was also prolonged[1]. |
别名 | Sephin 1, lcerguastat, IFB-088 |
分子量 | 196.64 |
分子式 | C8H9ClN4 |
CAS No. | 951441-04-6 |
Smiles | C(=N/NC(=N)N)\C1=C(Cl)C=CC=C1 |
密度 | 1.35 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 200 mg/mL (1017.10 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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