| Stereochemistry | RACEMIC |
| Molecular Formula | C15H22N2O3 |
| Molecular Weight | 278.3468 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCOC1=CC(CC2CNC(=O)N2)=CC=C1OC
InChI
InChIKey=PDMUULPVBYQBBK-UHFFFAOYSA-N
InChI=1S/C15H22N2O3/c1-3-4-7-20-14-9-11(5-6-13(14)19-2)8-12-10-16-15(18)17-12/h5-6,9,12H,3-4,7-8,10H2,1-2H3,(H2,16,17,18)
RO-20-1724 is a potent inhibitor of Phosphodiesterase 4 (PDE4) originally developed by Roche. It showed some promise as a potential treatment for psoriasis, but it was discontinued when it could not match the efficacy of existing treatments. RO-20-1724 was also investigated as a potential treatment for asthma and septic shock.
CNS Activity
Originator
Approval Year
Doses
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Tox targets
Sourcing
PubMed
Sample Use Guides
In a clinical trial for the treatment of psoriasis, a 1% RO-20-1724 cream was applied 4 times a day for 4 weeks to affected areas. RO-20-1724 was not as effective as intensive occlusive treatment of psoriatic lesions with 0.025% triamcinolone acetonide
Route of Administration:
Topical
Aortic vascular smooth muscle (VSM) cells were harvested from enzymatically dissociated rat thoracic aorta. Cells were stimulated by incubation with interleukin-lp (IL-10) at different concentrations for varying periods of time up to 48 h, with and without RO-20-1724. Nitric Oxide Synthase activity was assessed by measurement of nitrite production. RO-20-1724 had no detectable effect on nitrite levels in the absence of IL-lp but enhanced the production of nitrite in response to IL-Il in a dose-dependent manner.
ACTIVE MOIETY
