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Cilastatin sodium

Cat. No. 2709

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Alternative Name: MK 0791

Chemical Name: (2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic acid sodium salt

Biological Activity

Dipeptidase inhibitor (LTDase, leukotriene D4 hydrolase, dehydropeptidase I) that displays a K_i value of 0.11 μM. Inhibits metabolism of LTD₄ to LTE₄ and the hydrolysis of β-lactam antibiotics. Nephroprotective; reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells.

Technical Data

M.Wt:

380.43

Formula:

C₁₆H₂₅N₂NaO₅S

Solubility:

Soluble to 100 mM in water and to 10 mM in DMSO

Purity:

>99 %

Storage:

Desiccate at -20°C

CAS No:

81129-83-1

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Graham et al (1987) Inhibition of the mammalian β-lactamase renal dipeptidase (dehydropeptidase-I) by (Z)-2-(acylamino)-3-substituted-propenoic acids. J.Med.Chem. 30 1074. PMID: 3495664.

White et al (1999) A continuous fluorometric assay for leukotriene D₄ hydrolase. Anal.Biochem. 268 245. PMID: 10075814.

Perez et al (2004) Inhibition of brush border dipeptidase with cilastatin reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells. Nephrol.Dial.Transplant. 19 2445. PMID: 15252165.

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Keywords: Cilastatin sodium, supplier, Dipeptidase, LTDase, leukotrienes, eicosanoids, D4, hydrolase, dehydropeptidase, I, inhibitors, metabolism, LTD4, LTE4, Proteases, Proteinases, MK0791