PF-01247324 NEW
| Price | $67 | $112 | $243 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PF-01247324 | CAS No.: 875051-72-2 |
| Purity: 99.47% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PF-01247324 |
| Description | PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker [IC50: 196 nM]. |
| Animal Research | Rats: . For male Sprague Dawley rats (170-300?g), PF-01247324 is formulated as solutions of 0, 10, 30, 100?mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioral testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted[1]. Mice: . PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of the vehicle[2]. |
| In vitro | PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50: 331 nM) and recombinantly expressed h Nav1.8 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 demonstrates that PF-01247324 reduces excitability in both rat and human DRG neurons and alters the action potential waveform [1]. |
| In vivo | PF-01247324 (100 mg/kg) reduces phase 2 flinching by 37%. 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (166.36 mM) |
| Keywords | PF01247324 | Sodium Channel | PF 01247324 | Na+ channels | Na channels | PF-01247324 | Inhibitor | inhibit |
| Inhibitors Related | Phenytoin sodium | Lidocaine Hydrochloride hydrate | Lidocaine | Valproic Acid | Butamben | Lidocaine hydrochloride | L-Aspartic aicd sodium | Mebeverine hydrochloride | Amitriptyline hydrochloride | Riluzole | Benzocaine | Nefopam hydrochloride |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Sodium Channel Targeted Library | Neuroprotective Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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