DMP 777|cas 157341-41-8|DC Chemicals

DMP 777|cas 157341-41-8|DC Chemicals

DMP 777(L-694458) is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

IC50 value:

Target: elastase

After iv dosing, L-694,458 exhibited similar pharmacokinetic parameters in rats and rhesus monkeys.

Product Name: DMP 777|Cat No: DC9434|Cas: 157341-41-8|Molecule Formular: C31H40N4O6|Molecule Weight: 564.6725|Other names: DMP 777

DMP 777(L-694458) is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
After iv dosing, L-694,458 exhibited similar pharmacokinetic parameters in rats and rhesus monkeys. The bioavailability of a 10 mg/kg oral dose was higher in rats (65%) than in rhesus monkeys (39%). In both species, concentrations of L-694,458 in plasma increased more than proportionally when the oral dose was increased from 10 mg/kg to 40 mg/kg. In monkeys a protracted plasma concentration-time profile was observed at 40 mg/kg, characterized by a delayed T(max) (8-24 hr) and a long terminal half-life (6 hr). DMP-777 dissipated a gastric tubulovesicle proton gradient without impairing the H/K-ATPase activity, consistent with its pharmacological action as a parietal cell-specific protonophore which could induce parietal cell necrosis through backwash of luminal acid into actively secreting cells.

For research only, not for human use!