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Mitapivat (AG-348)

Cat. No. M9034
Mitapivat (AG-348) Structure
Synonym:

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

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 150  USD150 In stock
50mg USD 450  USD450 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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

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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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