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cpha

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  • Inhibitors & Agonists
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Cilastatin
MK0791
T258382009-34-5
Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.
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Metallo-β-lactamase-IN-11
T79435
Metallo-β-lactamase-IN-11 (compound 5f), a potent inhibitor of Metallo-β-lactamases (MBLs), demonstrates efficacy against bacterial metallophyllactamase CphA with an IC50 value of 45 µM. At 10 µM, it inhibits NDM-1 by 49% and AIM-1 by 61%, indicating its potential for research on countering antibiotic resistance [1].
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Cilastatin-15N,d3
TMID-03872738376-83-3
Cilastatin-15N,d3 is a version of Cilastatin that is labeled with ^15N and deuterium. Cilastatin (MK0791) acts as a reversible competitive inhibitor of renal dehydropeptidase I, with an IC50 of 0.1 μM. It inhibits the bacterial metallo-beta-lactamase CphA with an IC50 of 178 μM. Cilastatin is utilized as an antibacterial adjunct.
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