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81129-83-1

81129-83-1 structure
81129-83-1 structure
  • Name: Cilastatin Sodium
  • Chemical Name: cilastatin sodium
  • CAS Number: 81129-83-1
  • Molecular Formula: C16H25N2NaO5S
  • Molecular Weight: 380.43500
  • Catalog: analytical chemistry Standard Pharmacopoeia Standards and Magazine Standards
  • Create Date: 2018-07-14 20:50:26
  • Modify Date: 2025-08-20 19:47:50
  • Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct[1][2][3].
Name cilastatin sodium
Synonyms 2-heptenoic acid, 7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-, monosodium salt, (2Z)-
[R-[R*,S*(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]-2-heptenoic Acid Monosodium Salt
MFCD01723687
W-13 hydrochloride
2-heptenoicacid,7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyclopropyl
Cilastatine
Cilastatin sodium salt
Natrium-(2R)-2-amino-3-{[(5Z)-6-carboxy-6-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hex-5-en-1-yl]sulfanyl}propanoat
Sodium (2R)-2-amino-3-{[(5Z)-6-carboxy-6-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hex-5-en-1-yl]sulfanyl}propanoate
Cilastatin Sodium
Sodium (2Z)-7-{[(2R)-2-amino-2-carboxyethyl]sulfanyl}-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoate
Sodium hydrogen 7-[(2-amino-2-carboxylatoethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]hept-2-enoate
Sodium 7-(2-amino-2-carboxy-ethyl)sulfanyl-2-(2,2-dimethylcyclopropyl)carbonylamino-hept-2-enoate
Sodium Cilastatin
(2R)-2-amino-3-{[(5Z)-6-carboxy-6-({[(1S)-2,2-diméthylcyclopropyl]carbonyl}amino)hex-5-én-1-yl]sulfanyl}propanoate de sodium
Sodium (2Z)-7-{[(2R)-2-amino-2-carboxyethyl]sulfanyl}-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)-2-heptenoate
monosodiumsalt,(r-(r*,s*(z)))-)carbonyl)amino)
2-Heptenoic acid, 7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-, sodium salt, (2Z)- (1:1)
EINECS 279-694-4
(2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoicacidsodiumsalt
(Z)-7-[(R)-2-Amino-2-carboxyethylthio]-2-[(S)-2,2-dimethylcyclopropylcarbonylamino]-2-heptenoic acid 1-sodium salt
Sodium (Z)-7-(((R)-2-amino-2-carboxyethyl)thio)-2-((S)-2,2-dimethylcyclopropanecarboxamido)-2-heptenoate
Description Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct[1][2][3].
Related Catalog
Target

IC50: 0.1 μM (Renal dehydropeptidase I); 178 μM (Bacterial metallob-lactamase enzyme CphA)[1]

In Vitro Cilastatin (200 μg/mL; 24 hours; RPTECs) treatment protects against Vancomycin-induced proximal tubule apoptosis and increases cell viability, without compromising the antimicrobial effect of Vancomycin[2]. Apoptosis Analysis[2] Cell Line: Renal proximal tubular epithelial cells (RPTECs) Concentration: 200 μg/mL Incubation Time: 24 hours Result: Significantly ameliorated Vancomycin-induced nuclear apoptosis.
In Vivo In a mouse model (female mice, strain CD-1, 20 g) of systemic infection, Imipenem plus Cilastatin can protect mice from S. aureus, E. coli, and P. aeruginosa infection[3].
References

[1]. Keynan S, et al. The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterialmetallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.

[2]. S Keynan, et al. The Renal Membrane Dipeptidase (Dehydropeptidase I) Inhibitor, Cilastatin, Inhibits the Bacterial Metallo-Beta-Lactamase Enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.

[3]. Blanca Humanes, et al. Protective Effects of Cilastatin Against Vancomycin-Induced Nephrotoxicity. Biomed Res Int. 2015;2015:704382.

[4]. P J Petersen, et al. In Vitro and in Vivo Activities of LJC10,627, a New Carbapenem With Stability to Dehydropeptidase I. Antimicrob Agents Chemother. 1991 Jan;35(1):203-7.
Boiling Point 655.5ºC at 760 mmHg
Molecular Formula C16H25N2NaO5S
Molecular Weight 380.43500
Flash Point 350.2ºC
Exact Mass 380.13800
PSA 157.85000
LogP 1.18910
Storage condition Desiccate at -20°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
MJ9650200
CHEMICAL NAME :
2-Heptenoic acid, 7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyc lopropyl)carbonyl) amino)-, monosodium salt, (R-(R*,S*(Z)))-
CAS REGISTRY NUMBER :
81129-83-1
LAST UPDATED :
199209
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C16-H25-N2-O5-S.Na
MOLECULAR WEIGHT :
380.48

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
5027 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6786 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985
Hazard Codes Xi
RTECS MJ9650200
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