PF-01247324
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $779 | Check With Us |
500mg | $1070 | Check With Us |
1g | $1605 | Check With Us |
Cat #: V4470 CAS #: 875051-72-2 Purity ≥ 98%
Description: PF-01247324 is a novel, potent, selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
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Molecular Weight (MW) | 330.60 |
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Molecular Formula | C13H10Cl3N3O |
CAS No. | 875051-72-2 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent |
Protocol | 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 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 shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential |
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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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 3.0248 mL | 15.1240 mL | 30.2480 mL | 60.4961 mL |
5mM | 0.6050 mL | 3.0248 mL | 6.0496 mL | 12.0992 mL |
10mM | 0.3025 mL | 1.5124 mL | 3.0248 mL | 6.0496 mL |
20mM | 0.1512 mL | 0.7562 mL | 1.5124 mL | 3.0248 mL |
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