PF-01247324

ChemicalBook > CAS DataBase List > 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

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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

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Safety

RIDADR: UN 2811 6.1 / PGIII

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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.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0274
Product name: PF-01247324
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $115
Updated: 2023/06/20

Sigma-Aldrich

Product number: PZ0274
Product name: PF-01247324
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $451
Updated: 2023/06/20

Cayman Chemical

Product number: 22111
Product name: PF-01247324
Purity: ≥98%
Packaging: 1mg
Price: $33
Updated: 2024/03/01

Cayman Chemical

Product number: 22111
Product name: PF-01247324
Purity: ≥98%
Packaging: 5mg
Price: $96
Updated: 2024/03/01

Cayman Chemical

Product number: 22111
Product name: PF-01247324
Purity: ≥98%
Packaging: 10mg
Price: $176
Updated: 2024/03/01

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PF-01247324 Chemical Properties,Usage,Production

Description

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.

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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PF-01247324 Suppliers

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875051-72-2, PF-01247324Related Search:

FORMANILIDE PF-06700841-TsOH PF-06700841 tosylate PF-06282999 PF 4618433 PF-06650833 PF-6260933 5-PyriMidinecarboxaMide, 4-[(2-Methylpropyl)aMino]-N-(phenylMethyl)-2-[4-[(tetrahydro-2H-pyran-3-yl)Methyl]-1-piperazinyl]- PF 04995274 PNU 100480 PF 05175157 PF-06281355 PF06869206

2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-

6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide

6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE

PF-1247324

6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE

PF01247324;PF 01247324

PF-01247324

133786

CS-2577

Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit

875051-72-2