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PF-01247324

Chemical Structure : PF-01247324

CAS No.: 875051-72-2

PF-01247324 (PF01247324, PF 01247324)

Catalog No.: PC-42355Not For Human Use, Lab Use Only.

PF-01247324 is a potent, selective and orally active Nav1.8 channel blocker with IC50 of 196 nM, inhibits native TTX-R currents in human DRG neurons with IC50 of 331 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-01247324 is a potent, selective and orally active Nav1.8 channel blocker with IC50 of 196 nM, inhibits native TTX-R currents in human DRG neurons with IC50 of 331 nM.
PF-01247324 displays >50-fold selectivity over Nav1.5, Nav1.2 and Nav1.7 channels.
PF-01247324 inhibits native TTX-R currents in small-diameter rodent DRG neurons with IC50 of 448 nM, reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential in vitro current clamp.
PF-01247324 demonstrates efficacy in both inflammatory and neuropathic pain models.

Physicochemical Properties

M.Wt 330.597
Formula C13H10Cl3N3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxamide, 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)-

References

1. Payne CE, et al. Br J Pharmacol. 2015 May;172(10):2654-70.

2. Shields SD, et al. PLoS One. 2015 Mar 6;10(3):e0119067.

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