Cilastatin sodium A dipeptidase inhibitor with nephroprotective effects

Cilastatin sodium (CAS 81129-83-1)

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Synonym: [R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2- [[(2,2-dimethylcyclopropyl)carbonyl]amino]-2- heptenoic acid monosodium salt
Application: A dipeptidase inhibitor with nephroprotective effects
CAS Number: 81129-83-1
Purity: ≥98%
Molecular Weight: 380.43
Molecular Formula: C16H25N2O5S•Na
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cilastatin is a dipeptidase inhibitor that specifically inhibits DPEP1 (dehydrodipeptidase I), a renal membrane-bound glycoprotein involved in the hydrolytic metabolism of penem and carbapenem β-lactam antibiotics. Cilastatin has been shown to inhibit leukotriene D4 hydrolase in porcine kidney microvillar membranes which inhibits the conversion of leukotriene D4 to leukotriene E4. Also, Cilastatin has been used to maintain the antibiotic activity of imipenem (sc-205350) through inhibiting dipeptidase activity. It has been reported that Cilastatin exhibits nephroprotective effects in cyclosporine A-induced nephrotoxicity in kidney proximal tubule epithelial cells and inhibits the bacterial metallo-β-lactamase, an enzyme responsible for bacterial resistance to β-lactam antibiotics.


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Physical State :
Solubility :
Soluble in water (25 mg/mL), DMSO (10 mg/mL), and methanol.
Storage :
Store at -20° C
Ki Data :
LTDase: Ki= 0.11 µM; leukotriene D4 hydrolase: Ki= 0.11 µM; dehydropeptidase I: Ki= 0.11 µM
pK Values :
pKa: 2.0, 4.4, 9.2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
PubChem CID :
EC Number :

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Certificate of Analysis

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