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PF-04885614

Name: PF-04885614
Brand: TargetMol
SKU: T12421
Rating: 4.5 (1 reviews)

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Catalog No. T12421Cas No. 1480833-70-2

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

PF-04885614

Copy Product Info

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Catalog No. T12421Cas No. 1480833-70-2

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	Inquiry	Inquiry
5 mg	$58	Inquiry	Inquiry
10 mg	$93	Inquiry	Inquiry
25 mg	$178	Inquiry	Inquiry
50 mg	$333	Inquiry	Inquiry
100 mg	$470	Inquiry	Inquiry
200 mg	$662	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$58	-	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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Product Introduction

PF-04885614 AI Summary

PF-04885614 exhibits potent bioactivity as a sodium channel blocker, significantly inhibiting various sodium channels (Nav1.1, Nav1.2, Nav1.6, Nav1.7, Nav1.8) in recombinant human cells, as well as in rat and cynomolgus monkey DRG neurons, showing selective potency towards certain subtypes. It also demonstrates inhibition of ion channel binding and has a moderate pKa value. The compound shows a moderate metabolic profile based on intrinsic clearance data in human liver microsomes and hepatocytes. Additionally, PF-04885614 demonstrates antiviral activity against SARS-CoV-2 by inhibiting the cytotoxicity of Caco-2 and VERO-6 cells at a concentration of 10 µM after 48 hours, with an inhibition rate of 2.76% and -0.21%, respectively, as assessed by high content imaging. It also exhibits 34.96% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM in a FRET assay with a peptide substrate. Moreover, PF-04885614 inhibits human HDAC6 enzyme activity, resulting in a 50.84% decrease using a commercial peptide substrate and a 3.83% increase using a custom peptide substrate..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

Chemical Properties

Molecular Weight	285.27
Formula	C₁₃H₁₄F₃N₃O
Cas No.	1480833-70-2
Smiles	CC(C)(N)c1ncc([nH]1)-c1ccc(OC(F)(F)F)cc1
Relative Density.	1.293 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: 240 mg/mL (841.31 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (17.53 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	3.5055 mL	17.5273 mL	35.0545 mL	175.2725 mL
5 mM	0.7011 mL	3.5055 mL	7.0109 mL	35.0545 mL
10 mM	0.3505 mL	1.7527 mL	3.5055 mL	17.5273 mL
20 mM	0.1753 mL	0.8764 mL	1.7527 mL	8.7636 mL
50 mM	0.0701 mL	0.3505 mL	0.7011 mL	3.5055 mL
100 mM	0.0351 mL	0.1753 mL	0.3505 mL	1.7527 mL

Calculator

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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