Chemical Property of 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide
Chemical Property:
- Boiling Point:477.7±45.0 °C(Predicted)
- PKA:6.56±0.46(Predicted)
- PSA：68.74000
- Density:1.460±0.06 g/cm3(Predicted)
- LogP:3.97160
- Storage Temp.:room temp
- XLogP3:3.6
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:3
- Rotatable Bond Count:2
- Exact Mass:328.988945
- Heavy Atom Count:20
- Complexity:358
- Purity/Quality:
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99%, *data from raw suppliers
6-Amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CNC(=O)C1=NC(=C(C=C1)C2=C(C(=CC(=C2)Cl)Cl)Cl)N
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Description
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.
