An allosteric activator of PKR
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Mitapivat

Item No. 43908

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[4-(cyclopropylmethyl)-1-piperazinyl]carbonyl]phenyl]-8-quinolinesulfonamide
CAS Number
1260075-17-9
Synonyms
  • AG-348
Molecular Formula
C24H26N4O3S
Formula Weight
450.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N1CCN(CC2CC2)CC1)C3=CC=C(NS(C4=CC=CC5=CC=CN=C45)(=O)=O)C=C3
InChi Code
InChI=1S/C24H26N4O3S/c29-24(28-15-13-27(14-16-28)17-18-6-7-18)20-8-10-21(11-9-20)26-32(30,31)22-5-1-3-19-4-2-12-25-23(19)22/h1-5,8-12,18,26H,6-7,13-17H2
InChi Key
XAYGBKHKBBXDAK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    Mitapivat is an allosteric activator of erythrocyte pyruvate kinase (PKR).1 It increases PKR activity and ATP levels in red blood cells isolated from patients with pyruvate kinase deficiency when used at a concentration of 10 µM. Mitapivat increases hematocrit and hemoglobin levels, decreases osmotic fragility, and reduces splenic erythrophagocytosis in a model of hereditary spherocytosis using protein 4.2 knockout (4.2-/-) mice.2 Formulations containing mitapivat have been used in the treatment of hemolytic anemia in patients with pyruvate kinase deficiency.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rab, M.A.E., Van Oirschot, B.A., Kosinski, P.A., 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 106(1), 238-249 (2021).

    2. Matte, A., Wilson, A.B., Gevi, F., et al. Mitapivat reprograms the RBC metabolome and improves anemia in a mouse model of hereditary spherocytosis. JCI Insight 8(20), e172656 (2023).