シラスタチンナトリウム

外観

白色～ほとんど白色粉末～結晶

用途

デヒドロペプチダーゼⅠ阻害 剤です。カルバペネム系抗生物質の補助剤と して使用され、これら抗生物質がデヒドロペ プチダーゼⅠによって水解されて不活性化す る作用を示します。

効能

増強薬 (抗生物質), デヒドロペプチダーゼI阻害薬

化学的特性

White or light yellow amorphous, hygroscopic powder.

使用

Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects.

定義

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.

一般的な説明

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.

生物活性

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.