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PF-01247324

PF-01247324 Structure
PF-01247324
  • CAS No.875051-72-2
  • Chemical Name:PF-01247324
  • 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
  • pka 6.56±0.46(Predicted)
  • form powder
  • color white to beige
  • UNSPSC Code 41121801
  • NACRES NA.77
Safety
  • RIDADR  :UN 2811 6.1 / PGIII
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordDanger
  • Hazard statements H301-H315-H319-H335
  • Precautionary statements P301+P310+P330-P302+P352-P305+P351+P338
PF-01247324 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: PZ0274
  • Product name : PF-01247324
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹10825
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: PZ0274
  • Product name : PF-01247324
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹43613.93
  • Updated: 2022/06/14
  • Buy: Buy

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.
  • 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].

  • 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
  • IC 50 Nav1.8
PF-01247324 Preparation Products And Raw materials
Raw materials
Preparation Products
PF-01247324 Suppliers
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PF-01247324 Spectrum
875051-72-2, PF-01247324Related Search:
  • 化学试剂
  • 抑制剂
  • TPF-0124732
  • 化合物PF01247324,10 MM DMSO 溶液
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  • 化合物PF01247324
  • 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
  • 875051-72-2
  • TPF-0124732
  • PF-01247324, 10 mM in DMSO
  • Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
  • CS-2577
  • 133786
  • PF01247324;PF 01247324
  • 6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE
  • PF-01247324
  • PF-1247324
  • 6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE
  • 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide
  • 2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-

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