Mitapivat_product_DataBase

Bioactivity

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].

Target

pyruvate kinase.

Invitro

Mitapivat (0.1 nM-100 µM; 16 h) activates WT PK-R in RBCs from healthy donors[1].Mitapivat (0.01 nM-10 µM; 16 h) promotes production of ATP in RBC cells in a dose-dependent manner[1]. Cell Viability Assay[1] Cell Line:

In Vivo

Mitapivat (50 mg/kg; p.o.; twice daily for 21 days) improves anemia in a mouse model for β-thalassemia[2]. Animal Model:

Name

Mitapivat

CAS

1260075-17-9

Formula

C24H26N4O3S

Molar Mass

450.55

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Mitapivat

CAS: 1260075-17-9 F: C24H26N4O3S W: 450.55