Mitapivat

Research use only, not for human use.

Mitapivat, also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.

Mitapivat, also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.

Cell Viability Assay Cell Line:RBC cellsConcentration: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.

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.

PKR-IN-1 | PKM2 activator 1020 | Mitapivat

Angiogenesis

Syk

PKM2

Cancer

——

1260075-17-9

450.56

C24H26N4O3S

>98% (HPLC)

DMSO : 50 mg/mL. 110.98 mM;

C1CC1CN1CCN(CC1)C(=O)c1ccc(cc1)NS(=O)(=O)c1cccc2c1nccc2

N-{4-[4-(cyclopropylmethyl)piperazine-1-carbonyl]phenyl}quinoline-8-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years