A glucokinase activator
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PF-04937319 (hydrate)

Item No. 30926

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N-dimethyl-5-[[2-methyl6-[[5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-2-pyrimidinecarboxamide, hydrate
Molecular Formula
C22H20N6O4 • XH2O
Formula Weight
432.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
SMILES
CN(C)C(C1=NC=C(OC2=C(C=C(C)O3)C3=CC(C(NC4=NC=C(C)N=C4)=O)=C2)C=N1)=O.O
InChi Code
InChI=1S/C22H20N6O4.H2O/c1-12-8-24-19(11-23-12)27-21(29)14-6-17-16(5-13(2)31-17)18(7-14)32-15-9-25-20(26-10-15)22(30)28(3)4;/h5-11H,1-4H3,(H,24,27,29);1H2
InChi Key
TZHWWOYEMHALRI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $119

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    10 mg

    $215

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-04937319 is an activator of glucokinase (EC50s = 174, 407, and 269 nM for the recombinant human, rat, and dog enzymes, respectively).1 It increases glucose-induced insulin secretion in isolated rat islets when used at concentrations of 4 and 12 µM.2 PF-04937319 (3-100 mg/kg) reduces postprandial plasma glucose levels in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Petterson, J.C., Litchfield, J., Neef, N., et al. The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies. Toxicol. Pathol. 42(4), 696-708 (2014).

    2. Pffefferkorn, J.A., Guzman-Perez, A., Oates, P.J., et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm. 2, 828-839 (2011).