≥98%(HPLC) , 875051-72-2
Synonym(s):
6-Amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxylic acid methylamide;6-Amino-N-methyl-5-(2,3,5-trichlorophenyl)-2-Pyridinecarboxamide;N-Methyl-6-amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide;PF 01247324;PF-1247324
CAS NO.:875051-72-2
Empirical Formula: C13H10Cl3N3O
Molecular Weight: 330.6
MDL number: MFCD28156579
Pack Size | Price | Stock | Quantity |
5mg | RMB1033.47 | In Stock |
|
25mg | RMB4165.50 | In Stock |
|
others | Enquire |
PRODUCT Properties
Boiling point: | 477.7±45.0 °C(Predicted) |
Density | 1.460±0.06 g/cm3(Predicted) |
storage temp. | room temp |
solubility | DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml |
pka | 6.56±0.46(Predicted) |
form | powder |
color | white to beige |
Description and Uses
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.
6-Amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide is a Nav1.8 modulators that demonstrate efficacy in preclinical models of neuropathic and inflammatory pain, attenuates nociception and sensory neuron excitability.
Safety
Symbol(GHS) | GHS06 |
Signal word | Danger |
Hazard statements | H301-H315-H319-H335 |
Precautionary statements | P301+P310+P330-P302+P352-P305+P351+P338 |
RIDADR | UN 2811 6.1 / PGIII |