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PF-5006739

Name: PF-5006739
Brand: TargetMol
SKU: T16507
Rating: 4.5 (1 reviews)

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Catalog No. T16507Cas No. 1293395-67-1

PF-5006739 is a potent and selective CK1δ/ε inhibitor with IC50 values of 3.9 nM and 17.0 nM, respectively.It can be used in the study of psychiatric disorders and exhibits low nanomolar in vitro potency against CK1δ/ε and high kinome selectivity.PF-5006739 dose-dependently reduces opioid-seeking behavior in rodent relapse models and improves glucose tolerance in mouse models of diet-induced obesity (DIO) and genetic obesity (ob/ob).

PF-5006739

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Catalog No. T16507Cas No. 1293395-67-1

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$228	5 days	5 days

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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

Bioactivity

Description	PF-5006739 is a potent and selective CK1δ/ε inhibitor with IC50 values of 3.9 nM and 17.0 nM, respectively.It can be used in the study of psychiatric disorders and exhibits low nanomolar in vitro potency against CK1δ/ε and high kinome selectivity.PF-5006739 dose-dependently reduces opioid-seeking behavior in rodent relapse models and improves glucose tolerance in mouse models of diet-induced obesity (DIO) and genetic obesity (ob/ob).
Targets&IC50	CK1δ:3.9 nM, CK1ε:17.0 nM
In vitro	PF-5006739 shows low nanomolar in vitro inhibitory activity against CK1δ/ε, with IC50 values of 3.9 and 17 nM [1]. Treatment with PF-5006739 at 0.4–50 μM for 5 days rapidly and dose-dependently induces mPER2::luc bioluminescence in WAT tissue explants [2].
In vivo	PF-5006739 (10 mg/kg/day, subcutaneous injection, once daily) significantly improves blood glucose status in DIO mice [2].

Chemical Properties

Molecular Weight	419.45
Formula	C₂₂H₂₂FN₇O
Cas No.	1293395-67-1
Smiles	FC1=CC=C(C=C1)C=2N=CN(C2C=3N=C(N=CC3)N)C4CCN(CC5=NOC=C5)CC4
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (190.73 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3841 mL	11.9204 mL	23.8407 mL	119.2037 mL
5 mM	0.4768 mL	2.3841 mL	4.7681 mL	23.8407 mL
10 mM	0.2384 mL	1.1920 mL	2.3841 mL	11.9204 mL
20 mM	0.1192 mL	0.5960 mL	1.1920 mL	5.9602 mL
50 mM	0.0477 mL	0.2384 mL	0.4768 mL	2.3841 mL
100 mM	0.0238 mL	0.1192 mL	0.2384 mL	1.1920 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