PF-01247324
- Product Name
- PF-01247324
- CAS No.
- 875051-72-2
- Chemical Name
- PF-01247324
- Synonyms
- 133786;CS-2577;PF-1247324;PF-01247324;PF01247324;PF 01247324;6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide;6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE;2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-;6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE;Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
- CBNumber
- CB42682530
- Molecular Formula
- C13H10Cl3N3O
- Formula Weight
- 330.6
- MOL File
- 875051-72-2.mol
PF-01247324 Property
- 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
Safety
- RIDADR
- UN 2811 6.1 / PGIII
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- PZ0274
- Product name
- PF-01247324
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $115
- Updated
- 2023/06/20
- Product number
- PZ0274
- Product name
- PF-01247324
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $451
- Updated
- 2023/06/20
- Product number
- 22111
- Product name
- PF-01247324
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $33
- Updated
- 2024/03/01
- Product number
- 22111
- Product name
- PF-01247324
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $96
- Updated
- 2024/03/01
- Product number
- 22111
- Product name
- PF-01247324
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $176
- Updated
- 2024/03/01
PF-01247324 Chemical Properties,Usage,Production
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.
Uses
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.
Biochem/physiol Actions
In humans, PF-01247324 [6-amino-5-(2, 3, 5-trichloro-phenyl)-pyridine-2-carboxylic acid methylamide] prevents native tetrodotoxin-resistant (TTX-R) currents in dorsal root ganglion (DRG) neurons.
Enzyme inhibitor
This novel oral NaV1.8 blocker (FW = 330.59 g/mol) attenuates nociception and neuronal excitability by selectively targeting voltage-gated sodium transporter NaV1.8, with much weaker action against NaV1.1, NaV1.2, NaV1.4, NaV1.5, NaV1.6, and NaV1.7 transporters. PF-01247324 inhibited native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50 = 331 nM) and in recombinantly expressed hNav 1.8 (IC50 = 196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav 1.5 channels (IC50 ~ 10 μM) and 65-100 greater selectivity over TTX-sensitive (TTX-S) channels (IC50 ~ 10-18 μM). Native TTX-R currents in small diameter rodent DRG neurons were inhibited with an IC50 of 448 nM, and the block of both human recombinant Nav1.8 and TTX-R from rat DRG neurons was both frequency and statedependent. Unlike previously published NaV1.8 blockers, PF-01247324 demonstrates frequency-dependence, and off-target frequency-dependence at other sodium channel subtypes may reduce its selectivity window. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324
PF-01247324 Preparation Products And Raw materials
Raw materials
Preparation Products
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