1. Metabolic Enzyme/Protease
  2. Pyruvate Kinase
  3. Mitapivat

Mitapivat  (Synonyms: AG-348)

Cat. No.: HY-12689 Purity: 99.85%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Mitapivat Chemical Structure

Mitapivat Chemical Structure

CAS No. : 1260075-17-9

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
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5 mg USD 120 In-stock
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10 mg USD 210 In-stock
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50 mg USD 650 In-stock
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100 mg USD 1040 In-stock
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Description

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].

IC50 & Target

pyruvate kinase[1][2][3].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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.
In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model)[2].
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)[2].
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.
Clinical Trial
Molecular Weight

450.55

Formula

C24H26N4O3S

CAS No.
SMILES

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

Shipping

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
Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (46.23 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2195 mL 11.0975 mL 22.1951 mL
5 mM 0.4439 mL 2.2195 mL 4.4390 mL
10 mM 0.2220 mL 1.1098 mL 2.2195 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.55 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.85%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mitapivat
Cat. No.:
HY-12689
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