UK-383367 is a procollagen C-proteinase inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.

Procollagen C proteinase:44 nM

UK-383367 is effective at penetrating human skin. [1] UK-383367 inhibits collagen deposition with IC50 of ~2 μM. UK-383367 has modest affinity for all the PDE-4 subtypes PDE-4a, PDE-4b, PDE-4c and PDE-4d with IC50 of 1.8 μM, 1.5 μM, 2.4 μM and 0.9 μM, respectively. [2] UK-383367 is a weakly acidic compound and lipophilic. [3]

Plasma protein binding values for UK-383367 in rat, dog and human are 95%, 93% and 94%, respectively. UK-383367 following incubation in rat plasma results in the half-life of 49?min. UK-383367 following single intravenous administration (2 mg/kg) to rat results in the plasma clearance of 157?mL min?1?kg?1, the volume of distribution of 12?L kg?1, and an elimination half-life of 0.8? hour. UK-383367 following single intravenous administration (0.5 mg/kg) to dog results in the plasma clearance of 35?mL min?1?kg?1, the volume of distribution of 4.6?L kg?1, and an elimination half-life of 1.5?hours. UK-383367 following oral administration (2 mg/kg) to dog results in Cmax of 110 ng/mL, Tmax of 0.5-1.5 hour and oral bioavilability of 13%. [3]