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Category: EnzymesarrowProteasesarrowOther Proteases
Cat.No. Product Name
2709 Cilastatin sodium
Alternative name(s): MK 0791
Price and Availability

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Cilastatin
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 Ki 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:

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M.Wt: 380.43
Formula: C16H25N2NaO5S
Storage: Desiccate at -20°C
Solubility: Soluble to 100 mM in Water and to 10 mM in DMSO
Purity: >99%
CAS No: [81129-83-1]

Resources:

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    • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    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. White et al (1999) A continuous fluorometric assay for leukotriene D4 hydrolase. Anal.Biochem. 268 245. 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.
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    Keywords: Cilastatin, Proteases, Dipeptidase Inhibitor, MK 0791, Tocris Bioscience
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