≥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

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
• form: powder
• pka: 6.56±0.46(Predicted)
• color: white to beige
• 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)
• InChIKey: HPIUHDCRVYDAEJ-UHFFFAOYSA-N
• SMILES: Clc1c(cc(cc1c2c(nc(cc2)C(=O)NC)N)Cl)Cl

Description and Uses

PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Na_v1.8 (IC₅₀ = 0.19 μM for human Na_v1.8). It is selective for Na_v1.8 over Na_v1.1, Na_v1.2, Na_v1.5, and Na_v1.7 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 Na_v1.8 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
• target organs: Respiratory system
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: WGK 3
• Storage Class: 6.1C - Combustible acute toxic Cat.3; toxic compounds or compounds which causing chronic effects
• Hazard Classifications: Acute Tox. 3 Oral; Eye Irrit. 2; Skin Irrit. 2; STOT SE 3