2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. LEO 39652

LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .

For research use only. We do not sell to patients.

LEO 39652 Chemical Structure

LEO 39652 Chemical Structure

CAS No. : 1445656-91-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1].

IC50 & Target[1]

PDE4D

3.8 nM (IC50)

TNF-α

6.0 nM (IC50)

PDE4A

1.2 nM (IC50)

PDE4B

1.2 nM (IC50)

PDE4C2

3.0 nM (IC50)

In Vitro

LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LEO 39652 Related Antibodies
In Vivo

LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1]. Pharmacokinetic Analysis
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3 male Sprague Dawley rats, 2 female Göttingen minipigs, 2 male Göttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys[1]
Dosage: Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg
Administration: Intravenous injection
Result: Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.
Clinical Trial
Molecular Weight

421.45

Formula

C23H23N3O5
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(C1(C2=NN3C(C4=CC5=C(C(OC5)=O)C=C4)=CC=C(OC)C3=N2)CC1)OCC(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (59.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3728 mL 11.8638 mL 23.7276 mL
5 mM 0.4746 mL 2.3728 mL 4.7455 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3728 mL 11.8638 mL 23.7276 mL 59.3190 mL
5 mM 0.4746 mL 2.3728 mL 4.7455 mL 11.8638 mL
10 mM 0.2373 mL 1.1864 mL 2.3728 mL 5.9319 mL
15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9546 mL
20 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.9660 mL
25 mM 0.0949 mL 0.4746 mL 0.9491 mL 2.3728 mL
30 mM 0.0791 mL 0.3955 mL 0.7909 mL 1.9773 mL
40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4830 mL
50 mM 0.0475 mL 0.2373 mL 0.4746 mL 1.1864 mL
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LEO 39652 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LEO 396521445656-91-6LEO39652LEO-39652Phosphodiesterase (PDE)atopicdermatitisskinInhibitorinhibitorinhibit

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