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PF-01247324

Catalog No. T4490   CAS 875051-72-2

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker (IC50: 196 nM).

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PF-01247324 Chemical Structure
PF-01247324, CAS 875051-72-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 67.00
10 mg In stock $ 112.00
25 mg In stock $ 243.00
50 mg In stock $ 447.00
100 mg In stock $ 673.00
1 mL * 10 mM (in DMSO) In stock $ 67.00
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Purity: 99.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker (IC50: 196 nM).
Targets&IC50 Nav1.8 channel:196 nM
In vitro 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 vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential [1].
In vivo PF-01247324 (100 mg/kg) reduces phase 2 flinching by 37%. There is a significant effect of 30 mg/kg of PF-01247324 in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively [1]. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control [2].
Animal Research Rats: . For male Sprague Dawley rats (170-300?g), PF-01247324 is formulated as solutions of 0, 10, 30, 100?mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioral testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted[1]. Mice: . PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of the vehicle[2].
Molecular Weight 330.6
Formula C13H10Cl3N3O
CAS No. 875051-72-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (166.36 mM)

TargetMolReferences and Literature

1. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. 2. Shields SD, et al. Oral administration of PF-201247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e2019067.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Ion Channel Inhibitor Library NO PAINS Compound Library Orally Active Compound Library Bioactive Compound Library Anti-Cancer Compound Library ReFRAME Related Library Anti-Cardiovascular Disease Compound Library Sodium Channel Blocker Library Target-Focused Phenotypic Screening Library

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Keywords

PF-01247324 875051-72-2 Membrane transporter/Ion channel Sodium Channel PF01247324 PF 01247324 Na+ channels Na channels Inhibitor inhibit inhibitor

 

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