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LEO 39652

Name: LEO 39652
Brand: TargetMol
SKU: T38002
Rating: 4.5 (1 reviews)

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Catalog No. T38002Cas No. 1445656-91-6

LEO 39652, a dual-soft PDE4 inhibitor, demonstrates potent inhibition of PDE4 subtypes A, B, C, and D with respective IC50 values of 1.2 nM, 1.2 nM, 3.0 nM, and 3.8 nM. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM, indicating its potential for topical Atopic dermatitis (AD) research [1].

LEO 39652

😃Good

Catalog No. T38002Cas No. 1445656-91-6

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

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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	LEO 39652, a dual-soft PDE4 inhibitor, demonstrates potent inhibition of PDE4 subtypes A, B, C, and D with respective IC50 values of 1.2 nM, 1.2 nM, 3.0 nM, and 3.8 nM. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM, indicating its potential for topical Atopic dermatitis (AD) research [1].
Targets&IC50	PDE4C2:3.0 nM (IC50), PDE4B:1.2 nM (IC50), TNF-α:6.0 nM (IC50), PDE4D:3.8 nM (IC50), PDE4A:1.2 nM (IC50)
In vitro	LEO 39652 exhibits significant unbound in vitro efficacy, as demonstrated by its capacity to inhibit LPS-induced TNF-α release in human peripheral blood mononuclear cells (PBMC) cultured in serum-free medium. Additionally, LEO 39652 demonstrates relatively high affinity for binding to human serum albumin[2].
In vivo	LEO 39652 is inactivated both in blood and liver (dual-soft) while remaining stable in the skin[1]. Pharmacokinetic analysis reveals that LEO 39652 exhibits total clearance (rats 930, minipigs 200, and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6, and monkey 6%) following intravenous administration (rats 0.075, minipigs 0.5, and monkeys 2.0 mg/kg)[1].

Chemical Properties

Molecular Weight	421.45
Formula	C₂₃H₂₃N₃O₅
Cas No.	1445656-91-6
Smiles	COc1ccc(-c2ccc3C(=O)OCc3c2)n2nc(nc12)C1(CC1)C(=O)OCC(C)C

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: 25 mg/mL (59.32 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3728 mL	11.8638 mL	23.7276 mL	118.6380 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL	23.7276 mL
10 mM	0.2373 mL	1.1864 mL	2.3728 mL	11.8638 mL
20 mM	0.1186 mL	0.5932 mL	1.1864 mL	5.9319 mL
50 mM	0.0475 mL	0.2373 mL	0.4746 mL	2.3728 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