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Chemical Structure| 81129-83-1 Chemical Structure| 81129-83-1

Structure of Cilastatin sodium
CAS No.: 81129-83-1

Chemical Structure| 81129-83-1

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Cilastatin sodium is a reversible competitive renal dehydropeptidase I inhibitor (IC50 = 0.1 µM) that also inhibits the bacterial metalloenzyme CphA (IC50 = 178 µM). It is used as an adjuvant to antibiotics.

Synonyms: MK0791 sodium

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Product Details of Cilastatin sodium

CAS No. :81129-83-1
Formula : C16H25N2NaO5S
M.W : 380.43
SMILES Code : O=C([O-])/C(NC([C@@H]1C(C)(C)C1)=O)=C/CCCCSC[C@H](N)C(O)=O.[Na+]
Synonyms :
MK0791 sodium
MDL No. :MFCD08459332

Safety of Cilastatin sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Porcine renal proximal tubular epithelial cells (RPTECs) 200 µg/mL 24 h Cilastatin significantly reduced gentamicin-induced apoptosis, as evidenced by preserved cell morphology and reduced cell detachment. Additionally, Cilastatin decreased caspase-3 activation and nucleosomal DNA fragmentation. Antioxidants (Basel). 2020 Sep 3;9(9):821
rabbit primary proximal tubule cells (rPTCs) 100 µM 10 min To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in rPTCs, results showed that Cilastatin significantly inhibited Imipenem uptake. Acta Pharm Sin B. 2019 Sep;9(5):986-996
hOAT3-HEK293 cells 100 µM 10 min To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in hOAT3-HEK293 cells, results showed that Cilastatin significantly inhibited Imipenem uptake. Acta Pharm Sin B. 2019 Sep;9(5):986-996
hOAT1-HEK293 cells 100 µM 10 min To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in hOAT1-HEK293 cells, results showed that Cilastatin significantly inhibited Imipenem uptake. Acta Pharm Sin B. 2019 Sep;9(5):986-996

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Kunming mice Diclofenac-induced acute kidney injury model Intraperitoneal injection 25-100 mg/kg Single dose, duration of 24 hours To evaluate the protective effect of Cilastatin on diclofenac-induced acute kidney injury. Results showed that Cilastatin reduced renal pathological changes, dysfunction, oxidative stress, and inflammation, and decreased the renal distribution of diclofenac and its metabolite DLF-AG. Br J Pharmacol. 2020 May;177(9):1933-1948.
Wistar rats Gentamicin-induced acute kidney injury model Intraperitoneal injection 150 mg/kg Once daily for 8 days Cilastatin significantly ameliorated gentamicin-induced renal dysfunction, including reductions in serum creatinine, blood urea nitrogen (BUN), and kidney injury molecule-1 (KIM-1) levels. Furthermore, Cilastatin reduced morphological kidney damage, apoptosis, oxidative stress, and inflammatory responses. Antioxidants (Basel). 2020 Sep 3;9(9):821
Wistar rats Cisplatin-induced nephrotoxicity model Intraperitoneal injection 150 mg/kg Once daily for 5 days Cilastatin significantly attenuated cisplatin-induced nephrotoxicity, including body weight loss, renal dysfunction (assessed by GFR, serum creatinine, and BUN), morphological renal lesions, apoptotic cell death, and lipid peroxidation. Additionally, Cilastatin restored cisplatin-induced alterations in renal lipid distribution. J Lipid Res. 2018 Sep;59(9):1561-1574
New Zealand white rabbits Imipenem-induced acute kidney injury model Intravenous injection 200 mg/kg Single dose, observed for 48 hours To evaluate the protective effect of Cilastatin on Imipenem-induced nephrotoxicity, results showed that Cilastatin significantly alleviated kidney injury. Acta Pharm Sin B. 2019 Sep;9(5):986-996

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL

 

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