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) [1].

Product Specifications

CAS Number

[1445656-91-6]

UNSPSC

12352005

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/leo-39652.html

Purity

99.51

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C23H23N3O5

Molecular Weight

421.45

References & Citations

[1]Jens Larsen, et al. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5- (1-oxo-3 H-isobenzofuran-5-yl) -[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel "Dual-Soft" PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis. J Med Chem. 2020 Dec 10;63 (23) :14502-14521.|[2]Stefan Eirefelt, et al. Evaluating Dermal Pharmacokinetics and Pharmacodymanic Effect of Soft Topical PDE4 Inhibitors: Open Flow Microperfusion and Skin Biopsies. Pharm Res. 2020 Nov 13;37 (12) :243.