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PF 04531083

Name: PF 04531083
Brand: TargetMol
SKU: T16514
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16514Cas No. 1079400-07-9

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

PF 04531083

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🥰Excellent

Purity: 99.85%

Catalog No. T16514Cas No. 1079400-07-9

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$228	In Stock	In Stock
50 mg	$347	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:99.85%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

PF 04531083 AI Summary

PF 04531083 exhibits potent inhibition of human Nav1.8, with an IC50 of 700.0 nM, and shows selective inhibition of human Nav1.8/beta1 with an IC50 of 190.0 nM. It also inhibits voltage-gated sodium channels in rat and human DRG neurons, with IC50 values ranging from 200.0 to 540.0 nM. In a rat model, the compound demonstrates a half-life of 3.9 hours at 1 mg/kg and a Tmax of 1.3 hours at 2 mg/kg. It has moderate oral bioavailability with an F value of 59.0% at 2 mg/kg. Additionally, PF 04531083 shows an antiallodynic effect in a rat tibial nerve transection-induced mechanical allodynia model at 40 mg/kg and has a favorable unbound plasma concentration (Fu = 0.2). Notably, it penetrates the blood-brain barrier with a ratio of drug level from CSF to unbound plasma concentration at 40 mg/kg of 0.75 and at 250 mg/kg of 0.33..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

Chemical Properties

Molecular Weight	357.79
Formula	C₁₇H₁₆ClN₅O₂
Cas No.	1079400-07-9
Smiles	COc1ccc(Cl)c(c1)-c1ccc(NC(=O)c2ccnn2C)nc1N
Relative Density.	1.41 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 120 mg/mL (335.39 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.18 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	2.7949 mL	13.9747 mL	27.9494 mL	139.7468 mL
5 mM	0.5590 mL	2.7949 mL	5.5899 mL	27.9494 mL
10 mM	0.2795 mL	1.3975 mL	2.7949 mL	13.9747 mL
20 mM	0.1397 mL	0.6987 mL	1.3975 mL	6.9873 mL
50 mM	0.0559 mL	0.2795 mL	0.5590 mL	2.7949 mL
100 mM	0.0279 mL	0.1397 mL	0.2795 mL	1.3975 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