2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-01247324

PF-01247324 

Cat. No.: HY-101383 Purity: 99.63%
COA Handling Instructions

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.

For research use only. We do not sell to patients.

PF-01247324 Chemical Structure

PF-01247324 Chemical Structure

CAS No. : 875051-72-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
5 mg USD 84 In-stock
10 mg USD 144 In-stock
25 mg USD 312 In-stock
50 mg USD 540 In-stock
100 mg USD 900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

PF-01247324 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PF-01247324

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.

IC50 & Target

IC50: 196 nM (hNav1.8)[1]
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-01247324 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

330.60

Appearance

Solid

Formula

C13H10Cl3N3O
CAS No.
SMILES

O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (90.74 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0248 mL 15.1240 mL 30.2480 mL
5 mM 0.6050 mL 3.0248 mL 6.0496 mL
10 mM 0.3025 mL 1.5124 mL 3.0248 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.63%

COA (249 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1][2]

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 behavioural 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 vehicle[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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PF-01247324 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Keywords:

PF-01247324875051-72-2PF01247324PF 01247324Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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