MedChemExpress - Model Cefsulodin sodium hydrate -1426397-23-0
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Cefsulodin sodium hydrate
MCE China：Cefsulodin sodium hydrate
Brand：MedChemExpress (MCE)
Cat. No.HY-13588B
CAS：1426397-23-0
Synonyms：SCE-129 sodium hydrate
Storage：Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM.
In Vitro：Cefsulodin sodium (0.5-64 mg/mL; 18 h) is active in minimum inhibitory concentrations (MICs) of 0.5-64 mg/mL, is about 16- to 32-fold more active than Carbenicillin (HY-B0525) against Psuedomonas aeruginosa[1]. Cefsulodin sodium (8-16 μg/mL; 4.5 h) is not hydrolyzed by the beta-lactamase induced in P. aeruginosa by growth in the presence of benzylpenicillin[1].
In Vivo：Cefsulodin sodium (1 g/kg/tag; i.p.; 5 d, 9 single doses with intervals of 12 h) shows a increasing excretion of tubule cells in the rat, as a measure of nephrotoxicity, and displays tubule toxic threshold doses of 250 mg/kg (s.c.; 12 d) with nine single doses[4].
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References：
[1]. King A, et al. In vitro antibacterial activity and susceptibility of cefsulodin, an antipseudomonal cephalosporin, to beta-lactamases. Antimicrob Agents Chemother. 1980 Feb;17(2):165-9. [Content Brief]
[2]. Gotoh N, et al. Resistance of Pseudomonas aeruginosa to cefsulodin: modification of penicillin-binding protein 3 and mapping of its chromosomal gene. J Antimicrob Chemother. 1990 Apr;25(4):513-23. [Content Brief]
[3]. He R, et al. Cefsulodin Inspired Potent and Selective Inhibitors of mPTPB, a Virulent Phosphatase from Mycobacterium tuberculosis. ACS Med Chem Lett. 2015 Nov 3;6(12):1231-5. [Content Brief]
[4]. Sack K, et al. Renal tolerance of imipenem/cilastatin and other beta-lactam antibiotics in rats. Infection. 1985;13 Suppl 1:S156-60. [Content Brief]
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