产品
编 号：F099640
分子式：C24H26N4O3S
分子量：450.55
分子式：C24H26N4O3S
分子量：450.55
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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50mg
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100mg
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结构图
CAS No: 1260075-17-9
产品详情
生物活性：
Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.
体内研究：
Mitapivat (50 mg/kg；口服；每天两次，持续 21 天) 改善 β-地中海贫血小鼠模型的贫血。Animal Model:WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model).
Dosage:50 mg/kg
Administration:In animal feedings; single daily for 3 weeks.
Result:Increased the expression of pyruvate kinase isoforms in both red cells and erythroid precursors from Hbbth3/+mice.Elevated pyruvate kinase activity in cells from Hbbth3/+mice, and markedly increased ROS level in erythrocytes.Increased the expression of PKM2 in polychromatic and orthochromatic erythroblasts of Hbbth3/+mice.
Animal Model:WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model).
Dosage:50 mg/kg
Administration:Oral gavage, twice daily for 21 days.
Result:Ameliorated ineffective erythropoiesis and anemia in Hbbth3/+ mice and increased ATP, reduced ROS production, as well as reduced markers of mitochondrial dysfunction associated with improved mitochondrial clearance.
体外研究：
Mitapivat (0.1 nM-100 μM；16 h) 激活健康供体红细胞中的 WT PK-R。 Mitapivat (0.01 nM-10 μM；16 h) 促进产生红细胞中的 ATP 呈剂量依赖性。
Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.
体内研究：
Mitapivat (50 mg/kg；口服；每天两次，持续 21 天) 改善 β-地中海贫血小鼠模型的贫血。Animal Model:WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model).
Dosage:50 mg/kg
Administration:In animal feedings; single daily for 3 weeks.
Result:Increased the expression of pyruvate kinase isoforms in both red cells and erythroid precursors from Hbbth3/+mice.Elevated pyruvate kinase activity in cells from Hbbth3/+mice, and markedly increased ROS level in erythrocytes.Increased the expression of PKM2 in polychromatic and orthochromatic erythroblasts of Hbbth3/+mice.
Animal Model:WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model).
Dosage:50 mg/kg
Administration:Oral gavage, twice daily for 21 days.
Result:Ameliorated ineffective erythropoiesis and anemia in Hbbth3/+ mice and increased ATP, reduced ROS production, as well as reduced markers of mitochondrial dysfunction associated with improved mitochondrial clearance.
体外研究：
Mitapivat (0.1 nM-100 μM；16 h) 激活健康供体红细胞中的 WT PK-R。 Mitapivat (0.01 nM-10 μM；16 h) 促进产生红细胞中的 ATP 呈剂量依赖性。
产品资料
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