2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-05198007

PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.

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

PF-05198007 Chemical Structure

PF-05198007 Chemical Structure

CAS No. : 1235406-19-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

PF-05198007 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771[1][2].

IC50 & Target

Nav1.7

 

In Vitro

PF-05198007 (30 nM) blocks on average 83.0 ± 2.7% of the total TTX-S current indicating that the major TTX-S conductance is carried through Nav1.7 channels in small-diameter mouse DRG neurons (n = 35)[1].

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

PF-05198007 Related Antibodies
In Vivo

PF-05198007 (1 or 10 mg/kg, orally) reduces the capsaicin flare response in WT, but not Nav1.7Nav1.8Cre mice[1].

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

Animal Model: Adult Male C57Bl/6J Wild type (WT) and Nav1.7Nav1.8Cre mice[1].
Dosage: 1 or 10 mg/kg.
Administration: Orally once.
Result: Reduced the flare response to capsaicin for the duration of the observation period (55 mins; Vehicle; 4930 ± 751 versus 1 and 10 mg/kg 1967 ± 472 and 2265 ± 382, respectively (n = 7), AUC, p < 0.05).
Molecular Weight

533.91

Formula

C19H12ClF4N5O3S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(C1=CC(Cl)=C(OC2=CC=C(C(F)(F)F)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (280.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8730 mL 9.3649 mL 18.7297 mL
5 mM 0.3746 mL 1.8730 mL 3.7459 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 3.75 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 3.75 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8730 mL 9.3649 mL 18.7297 mL 46.8244 mL
5 mM 0.3746 mL 1.8730 mL 3.7459 mL 9.3649 mL
10 mM 0.1873 mL 0.9365 mL 1.8730 mL 4.6824 mL
15 mM 0.1249 mL 0.6243 mL 1.2486 mL 3.1216 mL
20 mM 0.0936 mL 0.4682 mL 0.9365 mL 2.3412 mL
25 mM 0.0749 mL 0.3746 mL 0.7492 mL 1.8730 mL
30 mM 0.0624 mL 0.3122 mL 0.6243 mL 1.5608 mL
40 mM 0.0468 mL 0.2341 mL 0.4682 mL 1.1706 mL
50 mM 0.0375 mL 0.1873 mL 0.3746 mL 0.9365 mL
60 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7804 mL
80 mM 0.0234 mL 0.1171 mL 0.2341 mL 0.5853 mL
100 mM 0.0187 mL 0.0936 mL 0.1873 mL 0.4682 mL
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PF-05198007 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.

Keywords:

PF-051980071235406-19-5PF05198007PF 05198007Sodium ChannelNa channelsNa+ channelscapsaicinNav1.7channelInhibitorinhibitorinhibit

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