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PF-4191834

Cat. No. M8115
PF-4191834 Structure
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Biological Activity

PF-4191834 a selective, non-redox, non-iron chelating competitive inhibitor of 5-lipoxygenase effective in inflammation and pain.

Chemical Information
Molecular Weight 393.5
Formula C22H23N3O2S
CAS Number 1029317-21-2
Solubility (25°C) DMSO: 2 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] Feng Shen, et al. Electrophilic fluoroalkylthiolation induced diastereoselective and stereospecific 1,2-metalate migration of alkenylboronate complexes

[2] Przemysław Rzodkiewicz, et al. Esculetin reduces leukotriene B4 level in plasma of rats with adjuvant-induced arthritis

[3] Jaime L Masferrer, et al. Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain

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