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

LEO 39652 

Cat. No.: HY-131707 Purity: 99.11%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 495 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

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].

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

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].

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.
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)

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
10 mM 0.2373 mL 1.1864 mL 2.3728 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

LEO 39652LEO39652LEO-39652Phosphodiesterase (PDE)atopicdermatitisskinInhibitorinhibitorinhibit

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Product Name:
LEO 39652
Cat. No.:
HY-131707
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