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PF 05089771

Name: PF 05089771
Brand: TargetMol
SKU: T7502L
Price: 326 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7502LCas No. 1235403-62-9

Alias PF-05089771, PF05089771

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

PF 05089771

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Purity: 99.42%

Catalog No. T7502LAlias PF-05089771, PF05089771Cas No. 1235403-62-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$62	In Stock	In Stock
5 mg	$148	In Stock	In Stock
10 mg	$196	In Stock	In Stock
25 mg	$326	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$167	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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Batch Information

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Purity:99.42%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

PF 05089771 AI Summary

PF 05089771 exhibits potent bioactivity as an inhibitor of the NaV1.7 ion channel, with an IC50 of 11.0 nM in human NaV1.7 expressed in HEK293 cells and 8.0 nM in mouse Nav1.7 channels in an inactivated state. It also shows significant selectivity over other sodium channels, such as Nav1.5, and demonstrates a high plasma protein binding across multiple species: 99.76% in humans, 99.52% in dogs, 99.45% in rats, and 98.7% in mice. The compound has notable oral bioavailability, moderate volume of distribution, and relatively short half-life in rat and dog models. Pharmacokinetically, it has a log D value of 2.3, an acidic pKa of 6.2, intrinsic clearance of 5.62 µL.min-1.(10^6cells)-1 in human hepatocytes, and a clearance rate of 40.0 mL.min-1.kg-1. In terms of therapeutic potential, PF 05089771 shows analgesic effects, reducing formalin-induced paw flinching by 52.0% in Sprague-Dawley rats at 100 mg/kg. Additionally, it has moderate inhibitory activity against CYP2C9 (IC50 = 299.0 nM) and antiviral activity against SARS-CoV-2 with an IC50 greater than 20,000 nM..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.
Targets&IC50	CynNav1.7:12 nM (IC50), Nav1.7 (rat):171 nM (IC50), Nav1.7 (dog):13 nM (IC50), Nav1.7 (human):11 nM (IC50), Nav1.7 (mouse):8 nM (IC50)
Synonyms	PF-05089771, PF05089771

Chemical Properties

Molecular Weight	500.35
Formula	C₁₈H₁₂Cl₂FN₅O₃S₂
Cas No.	1235403-62-9
Smiles	Nc1n[nH]cc1-c1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1cscn1
Relative Density.	1.673 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 30 mg/mL (59.96 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4 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	1.9986 mL	9.9930 mL	19.9860 mL	99.9300 mL
5 mM	0.3997 mL	1.9986 mL	3.9972 mL	19.9860 mL
10 mM	0.1999 mL	0.9993 mL	1.9986 mL	9.9930 mL
20 mM	0.0999 mL	0.4997 mL	0.9993 mL	4.9965 mL
50 mM	0.0400 mL	0.1999 mL	0.3997 mL	1.9986 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