875051-72-2
875051-72-2 structure
- Name: PF-01247324
- Chemical Name: 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide
- CAS Number: 875051-72-2
- Molecular Formula: C13H10Cl3N3O
- Molecular Weight: 330.59700
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2017-09-19 14:09:59
- Modify Date: 2024-01-06 17:19:55
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PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
| Name | 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide |
|---|---|
| Synonyms |
2-Pyridinecarboxamide,6-amino-N-methyl-5-(2,3,5-trichlorophenyl)
PF-01247324 |
| Description | PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel. |
|---|---|
| Related Catalog | |
| Target |
IC50: 196 nM (hNav1.8)[1] |
| In Vitro | PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50=331 nM) and in recombinantly expressed h Nav1.8 channels (IC50=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50=10-18 μM). In vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential[1]. |
| In Vivo | Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models. PF-01247324 reduces phase 2 flinching by 37% at 100 mg/kg. There is a significant effect of 30 mg/kg of PF-01247324 in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively[1]. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control[2]. |
| Animal Admin | Rats: For male Sprague Dawley rats (170-300 g), PF-01247324 is formulated as solutions of 0, 10, 30, 100 mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted[1]. Mice: PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of vehicle[2]. |
| References |
| Molecular Formula | C13H10Cl3N3O |
|---|---|
| Molecular Weight | 330.59700 |
| Exact Mass | 328.98900 |
| PSA | 68.74000 |
| LogP | 3.97160 |
| Storage condition | 2-8℃ |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H315-H319-H335 |
| Precautionary Statements | P301 + P310 + P330-P305 + P351 + P338 |
| RIDADR | UN 2811 6.1 / PGIII |