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PF-05089771

Cat. No. M8988
PF-05089771 Structure
Size Price Availability Quantity
5mg USD 400 In stock
10mg USD 580 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PF-05089771 is a Nav1.7 channel blocker with IC50s of 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively. PF-05089771 exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. PF-05089771 blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.

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 500.35
Formula C18H12Cl2FN5O3S2
CAS Number 1235403-62-9
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.
Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042. PMID: 28682065.

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.
Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405. PMID: 27050761.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-05089771 supplier, Sodium Channel, inhibitors

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