PF-01247324

PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 µM for human Nav1.8). It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 µM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 µM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 µM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain. It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund's adjuvant (CFA), respectively.Formal Name: 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)-2-pyridinecarboxamide. CAS Number: 875051-72-2. Molecular Formula: C13H10Cl3N3O. Formula Weight: 330.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 329 nm. SMILES: ClC1=CC(Cl)=CC(C2=C(N)N=C(C(NC)=O)C=C2)=C1Cl. 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). InChi Key: HPIUHDCRVYDAEJ-UHFFFAOYSA-N.