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Mitapivat (AG-348)

Cat. No. M9034

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Mitapivat (AG-348) Structure
Synonym:

PKR-IN-1; PKM2 activator 1020; Pyrukynd; AG-348

Size Price Availability Quantity
5mg USD 95 In stock
10mg USD 150 In stock
50mg USD 450 In stock
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Quality Control & Documentation
Biological Activity

Mitapivat (AG-348) is the first-in-class, oral effective pyruvate kinase small molecule allosteric activator. Mitapivat (AG-348) is active against wild-type and various mutated PKR enzymes, and promotes healthy red blood cell generation by activating mutated PKR to increase ATP levels.

Chemical Information
Molecular Weight 450.55
Formula C24H26N4O3S
CAS Number 1260075-17-9
Form Solid
Solubility (25°C) DMSO ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Hanny Al-Samkari, et al. Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias

[2] Alessandro Matte, et al. The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model

[3] Minke A E Rab, et al. Decreased activity and stability of pyruvate kinase in sickle cell disease: a novel target for mitapivat therapy

[4] Minke A E Rab, 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

[5] Rachael F Grace, et al. Safety and Efficacy of Mitapivat in Pyruvate Kinase Deficiency

Related Pyruvate Kinase Products
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Monofluorophosphate is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irreversibly inhibits phosphorylase phosphatase with Ki of 0.5 mM.

PKM2-IN-1

PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.

TEPP-46

Ml-265 (TEPP-46) is an effective activator of pyruvate kinase M2 (PKM2). ML265 induces the more active tetrameric state of PKM2 and the X-ray co-crystal structure shows that the activator binds at the dimer-dimer interface between two subunits of PKM2. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine.

DASA-58

DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC90 of 680 nM, and an AC50 of 38 nM.

Etavopivat

Etavopivat, an oral erythrocyte pyruvate kinase activator, is being developed for sickle cell disease and other hemoglobinopathies, previously reported in 2019.

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Keywords: Mitapivat (AG-348), PKR-IN-1; PKM2 activator 1020; Pyrukynd; AG-348 supplier, Pyruvate Kinase, inhibitors, activators

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