PDE4-IN-10

Names

[ CAS No. ]:
2413564-66-4

[ Name ]:
PDE4-IN-10

Biological Activity

[Description]:

PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology

[Target]

PDE4B:7.01 ± 1.0 μM (IC50)

PDE4D

TNF-α


[In Vitro]

PDE4-IN-10 (compound 7a) shows 64.56% inhibition at 10 µM against PDE4B, 54% inhibition at 30 µM but 17% inhibition at 10 µM against PDE4D, indicating its selectivity (~3.8 fold) towards PDE4B over PDE4D[1].

[References]

[1]. Bta B, et al. Synthesis of 11,12-dihydro benzo[c]phenanthridines via a Pd-catalyzed unusual construction of isocoumarin ring/FeCl3-mediated intramolecular arene-allyl cyclization: First identification of a benzo[c]phenanthridine based PDE4 inhibitor - ScienceDirect. Bioorganic Chemistry. April 2020;97:103691.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H13N

[ Molecular Weight ]:
243.30

Related Compounds