Bioactivity | 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]. |
CAS | 582332-31-8 |
Formula | C26H24F3N3O4 |
Molar Mass | 499.48 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |