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    InvivoChem Cat #: V4470
    CAS #: 875051-72-2 Purity ≥98%

    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.  

    References: Br J Pharmacol. 2015 May;172(10):2654-70.PLoS One. 2015 Mar 6;10(3):e0119067.

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    Name: PF-01247324
    CAS#: 875051-72-2
    Chemical Formula: C13H10Cl3N3O
    Exact Mass: 328.9889
    Molecular Weight: 330.59
    Elemental Analysis: C, 47.23; H, 3.05; Cl, 32.17; N, 12.71; O, 4.84
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF-01247324; PF 01247324; PF01247324.
    IUPAC/Chemical Name: 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide
    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)
    SMILES Code: O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC

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


    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.


    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.


    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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