An Nav1.8 sodium channel blocker (IC50 = 0.19 μM for human Nav1.8); selective for Nav1.8 over Nav1.1

PF-01247324 – 25 mg

Brand:
Cayman
CAS:
875051-72-2
Storage:
-20
UN-No:
Non-Hazardous - /

PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} 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.{36847} 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.  

 

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Description

An Nav1.8 sodium channel blocker (IC50 = 0.19 μM for human Nav1.8); 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 ERG potassium channels (IC50 = 30 μM); blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM); reduces phase 2 flinching in a rat model of formalin-induced persistent pain at 100 mg/kg; increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and CFA-induced mechanical hyperalgesia, respectively

Formal name: 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)-2-pyridinecarboxamide

Synonyms: 

Molecular weight: 330.6

CAS: 875051-72-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Pain Research

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