Cilastatin sodium

Химические свойства

White or light yellow amorphous, hygroscopic powder.

Использование

Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects.

Определение

ChEBI: The monosodium salt of cilastatin. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin sodium is therefore administ red with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to microbiologically inactive and potentially nephrotoxic products.

Общее описание

Cilastatin sodium salt is off-white to yellowish-white, hygroscopic, amorphous compound. It is derivatized from heptenoic acid. Its molecular mass is 380.43 g.

Биологическая активность

Dipeptidase inhibitor (LTDase, leukotriene D4 hydrolase, dehydropeptidase I) that displays a K i value of 0.11 μ M. Inhibits metabolism of LTD 4 to LTE 4 and the hydrolysis of β -lactam antibiotics. Nephroprotective; reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells.