Cas No.: | 157341-41-8 |
Synonyms: | L-694458; DMP-777; DMP777 |
SMILES: | O=C(N[C@@H](C1=CC=C2OCOC2=C1)CCC)N3[C@@H](OC4=CC=C(C(N5CCN(C)CC5)=O)C=C4)C(CC)(CC)C3=O |
Formula: | C31H40N4O6 |
M.Wt: | 564.6725 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |