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 | EIPA | Amiloride hydrochloride | Monensin sodium salt | Carbamazepine | 5-(N,N-Hexamethylene)-amiloride | Riluzole | 20(S)-Ginsenoside Rg3 | Lidocaine | Amitriptyline hydrochloride | Cariporide | Lamotrigine | Ranolazine dihydrochloride | Flecainide acetate | Phenytoin | Zonisamide | Veratridine | Oxcarbazepine | A-803467 | Triamterene | Flunarizine dihydrochloride | Vinpocetine | QX-314 chloride | Dronedarone | Propafenone hydrochloride | Mexiletine hydrochloride | Topiramate

品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
• 设有专业的实验中心和严格的质控、验证体系；
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
• 产品的生物活性多经各国客户实验验证；
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。