PF-01247324

Alias: PF-01247324; PF 01247324; PF01247324.
Cat No.:V4470 Purity: ≥98%
PF-01247324 is a novel, potent, selective and orally bioavailableNav1.8channel blocker with anIC50of 196 nM for recombinant human Nav1.8 channel.
PF-01247324 Chemical Structure CAS No.: 875051-72-2
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PF-01247324 is a novel, potent, selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel. PF-01247324 was administered by oral gavage at 1000 mg/kg; control groups received an equal volume of vehicle. Behavioral assays of motor coordination, grip strength, and ataxia were performed. We observed significant improvements in motor coordination and cerebellar-like symptoms in mice that received PF-01247324 compared to control littermates that received vehicle. These preclinical proof-of-concept data suggest that PF-01247324, its derivatives, or other Nav1.8-selective blockers merit further study for providing symptomatic therapy for cerebellar dysfunction in MS and related disorders. NaV 1.8 ion channels have been highlighted as important molecular targets for the design of low MW blockers for the treatment of chronic pain.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In human dorsal root ganglion (DRG) neurons, PF-01247324 inhibits both native tetrodotoxin-resistant (TTX-R) currents (IC50=331 nM) and recombinantly expressed hNav1.8 channels (IC50=196 nM). The selectivity of PF-01247324 is 50 times higher than that of the recombinantly expressed TTX-R hNav1.5 channel (IC50=10 μM), and 65–100 times higher than that of the TTX-sensitive (TTX-S) channel (IC50=10–18 μM). PF-01247324 was shown to alter the action potential waveform and decrease excitability in both rat and human DRG neurons by in vitro current clamp [1].
ln Vivo
Its effectiveness in neuropathic pain and inflammatory models was shown in rodent trials. At 100 mg/kg, PF-01247324 decreased phase 2 withdrawal by 37%. PF-01247324, at a dose of 30 mg/kg, significantly mitigates the effects of carrageenan-induced heat hyperalgesia and CFA-induced mechanical hyperalgesia in rat models [1]. When PF-01247324 was administered to mice instead of controls, there were notable improvements in motor coordination and cerebellar-like symptoms [2].
References
[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-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H10N3OCL3
Molecular Weight
330.597
CAS #
875051-72-2
SMILES
O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC
InChi Key
HPIUHDCRVYDAEJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H10Cl3N3O/c1-18-13(20)10-3-2-7(12(17)19-10)8-4-6(14)5-9(15)11(8)16/h2-5H,1H3,(H2,17,19)(H,18,20)
Chemical Name
6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide
Synonyms
PF-01247324; PF 01247324; PF01247324.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 30 mg/mL (~90.74 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0248 mL 15.1240 mL 30.2480 mL
5 mM 0.6050 mL 3.0248 mL 6.0496 mL
10 mM 0.3025 mL 1.5124 mL 3.0248 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Biological Data
  •  PF-01247324


    PF-01247324 is a selective Nav1.8 channel subtype-selective inhibitor.

     PF-01247324

    Antiallodynic effects of PF-01247324 in neuropathic pain. PF-01247324 reduced tactile allodynia in a spinal nerve ligation model (L5) of nerve injury.Br J Pharmacol. 2015 May; 172(10): 2654–2670.

  •  PF-01247324


    Inhibition by PF-01247324 is both use and state dependent at hNav1.8 channels and TTX-R in rat DRG neurons. Block of recombinant hNav1.8 and native TTX-R channels by PF-01247324 was assessed using voltage protocols designed to vary the amount of steady-state inactivation.

  •  PF-01247324


    Potency and selectivity for Nav1.8 channels can be achieved at the LA binding site.Br J Pharmacol. 2015 May; 172(10): 2654–2670.

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