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PF-05186462

Name: PF-05186462
Brand: TargetMol
SKU: T8711
Price: 126 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8711Cas No. 1235406-03-7

Alias PF-05150122

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

PF-05186462

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Purity: 99.37%

Catalog No. T8711Alias PF-05150122Cas No. 1235406-03-7

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$126	In Stock	In Stock
5 mg	$302	In Stock	In Stock
10 mg	$453	In Stock	In Stock
25 mg	$747	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$388	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.37%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

PF-05186462 AI Summary

PF-05186462 inhibits the NaV1.7 ion channel with an IC50 value of 13.0 nM and exhibits high plasma protein binding of 98.0%, indicating that a significant portion of the compound is bound to blood proteins. The compound has a LogD7.4 value of 1.15, suggesting its partitioning ability between octan-1-ol and water at pH 7.4. It shows bioactivities related to the inhibition of sodium channels (NaV), with varying levels of potency across different NaV subtypes: significant inhibition against NaV1.7 (IC50 = 21.0 nM), NaV1.2 (IC50 = 398.0 nM), and dog NaV1.7 (IC50 = 132.0 nM), but lower activity against NaV1.1 (IC50 = 8750.0 nM), NaV1.6 (IC50 = 1109.0 nM), and rat NaV1.7 (IC50 = 5450.0 nM). PF-05186462 also demonstrates moderate selectivity in inhibiting CYP2C9 (IC50 = 1101.0 nM) compared to CYP3A4, with favorable solubility and permeability properties for potential oral bioavailability in humans. Additional characteristics include an acidic pKa of 4.1, apparent permeability of 0.8 x 10^-6 cm/s in dog MDCKII-LE cells at pH 7.4, log D value of 0.8 at pH 7.4, low fraction unbound in rat plasma (Fu = 0.000221) and human plasma (Fu = 0.000016), differential blood/plasma drug level ratios for Wistar Hannover rat (0.67) and humans (0.66) after intravenous dosing, and hepatic clearance values of 40.3 mL.min^-1.kg^-1 in Wistar Hannover rats and 1.3 mL.min^-1.kg^-1 in humans..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.
Targets&IC50	Nav1.7 (human):21 nM (IC50)
Synonyms	PF-05150122

Chemical Properties

Molecular Weight	531.89
Formula	C₁₉H₁₀ClF₄N₅O₃S₂
Cas No.	1235406-03-7
Smiles	O(C1=C(C=C(C(F)(F)F)C=C1)C=2C=CN=NC2)C3=C(Cl)C=C(S(NC4=NN=CS4)(=O)=O)C(F)=C3
Relative Density.	1.629 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 11 mg/mL (20.68 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.76 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8801 mL	9.4004 mL	18.8009 mL	94.0044 mL
5 mM	0.3760 mL	1.8801 mL	3.7602 mL	18.8009 mL
10 mM	0.1880 mL	0.9400 mL	1.8801 mL	9.4004 mL
20 mM	0.0940 mL	0.4700 mL	0.9400 mL	4.7002 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc