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PF 04991532

Cat. No. M7116
PF 04991532 Structure
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Biological Activity

PF 04991532 is a potent hepatoselective glucokinase activator (EC50 = 90 nM). Exhibits >50-fold liver to pancreas ratio of tissue distribution. Reduces fasting and postprandial glucose levels with no hypoglycemia in a rat diabetes model.

Chemical Information
Molecular Weight 396.36
Formula C18H19F3N4O3
CAS Number 1215197-37-7
Solubility (25°C) DMSO 39.64 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] Wright, et al. Neuron. The lipid kinase PIP5K1C regulates pain signaling and sensitization.

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Keywords: PF 04991532 supplier, Glucokinase (GK), inhibitors, activators


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