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PF-05089771 Tosylate

Cat. No. M8092
PF-05089771 Tosylate Structure
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PF-05089771 Tosylate is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. PF-05089771 targets the voltage-sensing domain, preferentially interacting with, and stabilizing, inactivated channel conformations by interaction with the voltage-sensor domain (VSD) of Domain 4. Nav1.7 is expressed in sensory neurons and is critical for pain processing. PF-05089771 is being investigated for the treatment of chronic neuropathic pain.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 672.56
Formula C18H12Cl2FN5O3S2 · C7H8O3S
CAS Number 1430806-04-4
Purity >98%
Solubility DMSO: 30 mg/mL
clear
Storage at -20°C
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PF-05089771

PF-05089771 is a selective Nav1.7 channel blocker that interacts with the voltage-sensor domain (VSD) of domain IV.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-05089771 Tosylate supplier, Sodium Channel, inhibitors

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