Mitapivat

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[1][2][3].

Product Specifications

CAS Number

[1260075-17-9]

Product Name Alternative

AG-348

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Pyruvate Kinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/PKR-IN-1.html

Purity

99.97

Solubility

DMSO : 20.83 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=C2N=CC=CC2=CC=C1)(NC3=CC=C(C(N4CCN(CC5CC5)CC4)=O)C=C3)=O

Molecular Formula

C24H26N4O3S

Molecular Weight

450.55

Precautions

H315, H319, H320

References & Citations

[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.