Molecular Formula | C15H24N4O4 |
Molar Mass | 324.38 |
Density | 1.233 |
Melting Point | 136-138℃ |
Solubility | DMSO: >30mg/mL |
Appearance | powder |
Color | white to off-white |
pKa | 9.03±0.20(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
MDL | MFCD19690945 |
Use | UK-383,367 |
In vitro study | UK-383367 effective penetration of human skin. UK-383367 inhibited collagen deposition with an IC50 of ~ 2 μm. UK-383367 has modest affinity for all PDE-4 subtypes, with IC50 values of 1.8 μm, 1.5 μm, 2.4 μm and 0.9 μm for PDE-4a, PDE-4b, PDE-4c and PDE-4d, respectively. UK-383367 is a weakly acidic compound that is lipophilic. |
In vivo study | The plasma protein binding values of UK-383367 for rats, dogs and humans were 95%,93% and 94%, respectively. UK-383367 was incubated in rat plasma with a half-life of 49 minutes. UK-383367 at a dose of 2 mg/kg administered intravenously alone in rats with a plasma clearance of 157 μm min |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.083 ml | 15.414 ml | 30.828 ml |
5 mM | 0.617 ml | 3.083 ml | 6.166 ml |
10 mM | 0.308 ml | 1.541 ml | 3.083 ml |
5 mM | 0.062 ml | 0.308 ml | 0.617 ml |
biological activity | UK 383367 is a procollagen C- proteinase (procollagen C- terminal protease) inhibitor with IC50 of 44 nM and excellent selectivity for MMPs. |
target | TargetValue Procollagen C proteinase 44 nM |
Target | Value |
Procollagen C proteinase | 44 nM |
in vitro study | UK-383367 effectively penetrates human skin. UK-383367 inhibits collagen deposition with IC50 of ~ 2 μM. UK-383367 has a moderate affinity for all PDE-4 subtypes, acting on 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. UK-383367 is a weakly acidic compound with lipophilicity. |
In vivo studies | The plasma protein binding values of UK-383367 on rats, dogs and humans are 95%,93% and 94% respectively. UK-383367 was incubated in rat plasma with a half-life of 49 minutes. UK-383367 rats were treated intravenously at a dose of 2 mg/kg, and the plasma clearance rate was 157 mL min |