产品
编 号：F535915
分子式：C8H9ClN4
分子量：196.64
分子式：C8H9ClN4
分子量：196.64
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 951441-04-6
产品详情
生物活性：
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.
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.
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。
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.
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.
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。
产品资料
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