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PF-01247324

Cat. No. M8947
PF-01247324 Structure
Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 560 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PF-01247324 is a novel selective and orally bioavailable Nav 1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel. PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50=331 nM) and in recombinantly expressed h Nav1.8 channels (IC50=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50=10-18 μM).

In vivo, PF-01247324 (30 mg/kg) showed significant effect in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mice
Formulation suspended in 0.5% methylcellulose, 0.1% Tween 80
Dosages 1000 mg/kg in a volume of 10 mL/kg
Administration oral gavage
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 330.6
Formula C13H10Cl3N3O
CAS Number 875051-72-2
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis.
Shields SD, et al. PLoS One. 2015 Mar 6;10(3):e0119067. PMID: 25747279.

A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.
Payne CE, et al. Br J Pharmacol. 2015 May;172(10):2654-70. PMID: 25625641.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-01247324 supplier, Sodium Channel, inhibitors

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