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S9106314

≥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
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Update time: 2022-07-08

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

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