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PF-05198007 

Cat. No. M28007
PF-05198007  Structure
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Biological Activity

PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.

Chemical Information
Molecular Weight 533.91
Formula C19H12ClF4N5O3S2
CAS Number 1235406-19-5
Form Solid
Solubility (25°C) DMSO 150 mg/mL (ultrasonic)
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] George Goodwin, et al. Pain. Examination of the contribution of Nav1.7 to axonal propagation in nociceptors

[2] Aristos J Alexandrou, et al. PLoS One. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-05198007  supplier, Sodium Channel, inhibitors, activators


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