Cilastatin sodium - CAS 81129-83-1
Catalog number: B0084-077802
Category: Inhibitor
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Molecular Formula:
C16H25N2NaO5S
Molecular Weight:
380.43
COA:
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Targets:
Leukotriene Receptor
Description:
Cilastatin sodium is the sodium salt of cilastatin, which is a dipeptidase inhibitor of renal enzyme dehydropeptidase-I and leukotriene D4 peptidase. It inhibits metabolism of LTD4 to LTE4 and the hydrolysis of β-lactam antibiotics. It reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells. It can be combined intravenously with imipenem in order to protect it from dehydropeptidase. It suppresses both host and target metabolism of the broad-spectrum antibiotic imipenem, improving its efficacy. It usually confers antibiotic resistance to certain bacteria because itself does not have antibiotic activity. It has nephroprotective effects.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-077802 1 g $550 In stock
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Purity:
≥99% by HPLC
Synonyms:
L 642957; MK 791; L642957; MK791; L-642957; MK-791; [R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]-2-heptenoic Acid Monosodium Salt; (2Z)​-7-​[[(2R)​-​2-​Amino-​2-​carboxyethyl]​thio]​-​2-​[[[(1S)​-​2,​2-​dimethylcyclopropyl]​carbonyl]​amino]​-​2-heptenoic Acid Sodium Salt; sodium S-((Z)-6-carboxy-6-((S)-2,2-dimethylcyclopropane-1-carboxamido)hex-5-en-1-yl)-L-cysteinate
MSDS:
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InChIKey:
QXPBTTUOVWMPJN-QBNHLFMHSA-M
InChI:
InChI=1S/C16H26N2O5S.Na/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21;/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23);/q;+1/p-1/b12-6-;/t10-,11+;/m1./s1
Canonical SMILES:
CC1(CC1C(=O)NC(=CCCCCSCC(C(=O)O)N)C(=O)[O-])C.[Na+]
1.[Comparison of the modified Hodge test and the Carba NP test for detection of carbapenemases in Enterobacteriaceae isolates].
Bayramoğlu G1, Uluçam G, Gençoğlu Özgür Ç, Kılıç AO, Aydın F. Mikrobiyol Bul. 2016 Jan;50(1):1-10.
A rapid, practical, and accurate identification of carbapenemase-producing Enterobacteriaceae isolates is crucial for the implementation of appropriate infection control measures and proper treatment of the infections. For this purpose, a large number of phenotypic test methods have been developed, although none has 100% sensitivity and specificity. Variations in sensitivity and specificity of these tests based on the type of beta-lactamase enzymes carried by that isolates might result in differences between regions and countries. The aim of this study was to compare the performances of widely used modified Hodge test (MHT) and Carbapenemase Nordmann-Poirel (Carba NP) test in the detection of carbapenemases in Enterobacteriaceae family members. A total of 65 Enterobacteriaceae isolates (43 bla(OXA-48), 10 bla(VIM), 9 bla(IMP), 1 bla(NDM-1), 1 bla(KPC-2) and 1 bla(OXA-48)+bla(VIM) carrying strains) that showed decreased sensitivity to at least one carbapenem (ertapenem, imipenem or meropenem), and carriage of carbapenemase gene confirmed by polymerase chain reaction (PCR), were included in the study.
2.Molecular detection and antimicrobial resistance of Klebsiella pneumoniae from house flies (Musca domestica) in kitchens, farms, hospitals and slaughterhouses.
Ranjbar R1, Izadi M2, Hafshejani TT3, Khamesipour F4. J Infect Public Health. 2016 Feb 11. pii: S1876-0341(16)00003-4. doi: 10.1016/j.jiph.2015.12.012. [Epub ahead of print]
Identifying disease vectors and pathogens is one of the key steps in controlling vector-borne diseases. This study investigated the possible role of house flies (Musca domestica) as vectors in the transmission of Klebsiella pneumoniae in Chaharmahal VA Bakhtiari and Isfahan provinces of Iran. House flies were captured from household kitchens, cattle farms, chicken farms, animal hospitals, human hospitals and slaughterhouses. Isolation of K. pneumoniae from external surfaces and guts of the flies was performed using MacConkey agar (MA) and thioglycollate broth (TGB). Identification of the isolates was performed with phenotypic techniques and polymerase chain reaction (PCR). A total of 600 house flies were sampled during the study period from different locations in four different seasons. Overall, 11.3% of the captured house flies were positive for K. pneumoniae. In Chaharmahal VA Bakhtiari province, the prevalence was 12.7%, while in Isfahan province, 10.
3.Multi-drug resistant Pseudomonas aeruginosa keratitis and its effective treatment with topical colistimethate.
Chatterjee S1, Agrawal D. Indian J Ophthalmol. 2016 Feb;64(2):153-7. doi: 10.4103/0301-4738.179721.
The purpose was to evaluate the clinical outcome in multi-drug resistant Pseudomonas aeruginosa (MDR-PA) bacterial keratitis and report the successful use of an alternative antibiotic, topical colistimethate in some of them. The medical records of 12 culture-proven MDR-PA keratitis patients, all exhibiting in vitro resistance by Kirby-Bauer disc diffusion method to ≥ three classes of routinely used topical antibiotics were reviewed. Eight patients were treated with 0.3% ciprofloxacin or ofloxacin, 1 patient with 5% imipenem/cilastatin and 3 patients with 1.6% colistimethate. The outcomes in 8 eyes treated with only fluoroquinolones were evisceration in 4 eyes, therapeutic corneal graft in 1 eye, phthisis bulbi in 1 eye, and no improvement in 2 eyes. The eye treated with imipenem/cilastin required a therapeutic corneal graft. All the three eyes treated with 1.6% colistimethate healed. Colistimethate may prove to be an effective alternative antibiotic in the treatment of MDR-PA keratitis.
4.Imipenem/cilastatin-induced acute eosinophilic pneumonia.
Foong KS1, Lee A2, Pekez M2, Bin W3. BMJ Case Rep. 2016 Mar 4;2016. pii: bcr2016214804. doi: 10.1136/bcr-2016-214804.
Drugs, toxins, and infections are known to cause acute eosinophilic pneumonia. Daptomycin and minocycline are the commonly reported antibiotics associated with acute eosinophilic pneumonia. In this study, we present a case of imipenem/cilastatin-induced acute eosinophilic pneumonia. The patient presented with fever, acute hypoxic respiratory distress, and diffuse ground-glass opacities on the chest CT a day after the initiation of imipenem/cilastatin. Patient also developed peripheral eosinophilia. A reinstitution of imipenem/cilastatin resulted in recurrence of the signs and symptoms. A bronchoscopy with bronchoalveolar lavage showed 780 nucleated cells/mm(3) with 15% eosinophil. The patient's clinical condition improved significantly after the discontinuation of imipenem/cilastatin therapy and the treatment with corticosteroid.
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CAS 81129-83-1 Cilastatin sodium

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