UK-500001

UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM) . UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma[1].

Product Specifications

CAS Number

[582332-31-8]

UNSPSC

12352005

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/uk-500001.html

Smiles

O=C(C1=C(C=CC(C)=C1)O)N[C@H](CC2)CC[C@H]2NC(C(C=C(F)C=N3)=C3OC4=CC(F)=C(F)C=C4)=O

Molecular Formula

C26H24F3N3O4

Molecular Weight

499.48

References & Citations

[1]Moretto N, et al., CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration. J Pharmacol Exp Ther. 2015 Mar;352 (3) :559-67.