MK-789

MK-789 is a competitive reversible inhibitor of dehydropeptidase I (DHP-I). MK-789 competitively blocks the entry of N-formimidoylthienamycin into proximal tubular cells, thereby inhibiting its renal metabolism. MK-789 shifts the renal excretion pathway of N-formimidoylthienamycin to glomerular filtration only, increasing its urinary recovery rate and renal clearance. MK-789 is applicable to studies on renal metabolism and pharmacokinetics^[1]. In Vitro:MK-789 and its oxidative metabolites inhibit purified dehydropeptidase I in spectrophotometric assays^[1]. In Vivo:MK-789 (25, 75, 150 mg; intravenous injection; single administration; 7-day washout period between each dose) increases the urinary recovery rate of co-administered 150 mg N-formimidoylthienamycin to a plateau value of approximately 61% in healthy Caucasian male subjects; it elevates the plasma AUC of co-administered N-formimidoylthienamycin by approximately 20% without altering its plasma half-life^[1].\n