产品
编 号：F610736
分子式：C24H20N4O2
分子量：396.44
分子式：C24H20N4O2
分子量：396.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 864388-65-8
产品详情
生物活性：
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
体内研究：
MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection.MK-28 (1 mg/kg, IP, daily for 28 days) improves systemic function and survival in R6/2 mice and induces increased levels of eIF2α-P in the mouse brain striatum.MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity.Animal Model:R6/2 mice.
Dosage:1 mg/kg.
Administration:IP, daily for 28 days.
Result:Incerased the survival.
体外研究：
MK-28 (0-100 μM) shows PERK selectivity in vitro on a 391-kinase panel and rescues cells (but not PERK?/? cells) from ER stress-induced apoptosis.ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111 cells at high MK-28 concentration. CHOP and GADD34 mRNA levels show a signifcant increase in both cell types, up to 10- and 5-fold respectively.MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2).
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
体内研究：
MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection.MK-28 (1 mg/kg, IP, daily for 28 days) improves systemic function and survival in R6/2 mice and induces increased levels of eIF2α-P in the mouse brain striatum.MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity.Animal Model:R6/2 mice.
Dosage:1 mg/kg.
Administration:IP, daily for 28 days.
Result:Incerased the survival.
体外研究：
MK-28 (0-100 μM) shows PERK selectivity in vitro on a 391-kinase panel and rescues cells (but not PERK?/? cells) from ER stress-induced apoptosis.ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111 cells at high MK-28 concentration. CHOP and GADD34 mRNA levels show a signifcant increase in both cell types, up to 10- and 5-fold respectively.MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2).
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