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Mitapivat 99%

Mitapivat

MedMol
S82625
1260075-17-9
C24H26N4O3S
450.5533
品牌 貨號 產品規(guī)格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數(shù)量
MedMol S82625-1mg 99% ￥320.00元 5 - - -
MedMol S82625-5mg 99% ￥710.00元 4 - - -
MedMol S82625-10mg 99% ￥1130.00元 5 - - -
MedMol S82625-25mg 99% ￥1700.00元 5 - - -
MedMol S82625-50mg 99% ￥3000.00元 6 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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
產品描述： 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
靶點： pyruvate kinase;PKM
體外研究：
Mitapivat (0.1 nM-100 μM; 16 h) activates WT PK-R in RBCs from healthy donors. Mitapivat (0.01 nM-10 μM; 16 h) promotes production of ATP in RBC cells in a dose-dependent manner. Cell Viability Assay Cell Line: RBC cells Concentration: 0.1 nM-100 μM Incubation Time: 16 h (incubate overnight) Result: Increased PK-R activity in a dose-dependent manner to ~2.5-fold of DMSO control with an AC50 of 62 nM. Cell Viability Assay Cell Line: RBC cells Concentration: 0.01 nM-10 μM Incubation Time: 16 h (incubate overnight) Result: Consistently increased ATP levels in a dose-dependent manner by an average of 60% over DMSO control with an AC50 of 10.9 nM.
體內研究：
Mitapivat (50 mg/kg; p.o.; twice daily for 21 days) improves anemia in a mouse model for β-thalassemia. 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.
參考文獻：
1. Kung C, et al. AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency. Blood. 2017 Sep 14;130(11):1347-1356. 2. Matte A, et al. The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model. J Clin Invest. 2021 May 17;131(10):e144206. 3. Rab MAE, et al. AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Haematologica. 2021 Jan 1;106(1):238-249.
溶解性： Soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.219 ml 11.097 ml 22.195 ml
5 mM 0.444 ml 2.219 ml 4.439 ml
10 mM 0.222 ml 1.11 ml 2.219 ml
50 mM 0.044 ml 0.222 ml 0.444 ml
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參考文獻

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