PF-01247324

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PF-01247324

CAS No. : 875051-72-2

MCE 国际站：PF-01247324

产品活性：PF-01247324是选择性且有口服活性的Na_v1.8通道阻断物，对人类重组Na_v1.8 的IC₅₀值为196 nM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

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 Na_v1.8 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.

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. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control.

相关产品：Bioactive Compound Library Plus  |  Membrane Transporter/Ion Channel Compound Library  |  Orally Active Compound Library  |  Neuroprotective Compound Library  |  Targeted Diversity Library  |  Sodium Channel Blocker Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Ion Channel Compound Library  |  Amiloride hydrochloride  |  Halofuginone  |  Carbamazepine  |  Riluzole  |  20(S)-Ginsenoside Rg3  |  TPC2-A1-P  |  Lidocaine  |  Amitriptyline hydrochloride  |  Veratridine  |  5-(N,N-Hexamethylene)-amiloride  |  Triamterene  |  Fluphenazine dihydrochloride  |  Lamotrigine  |  Flunarizine dihydrochloride  |  QX-314 chloride  |  Phenytoin  |  A-803467  |  Ranolazine  |  Benzamil hydrochloride  |  Vinpocetine  |  Dronedarone  |  GS967  |  Metergoline  |  PF 05089771  |  Primidone  |  Propafenone hydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds