Cefiderocol-S-649266-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECefiderocolCat. No.: HY-17628CAS No.: 1225208-94-5Synonyms: S-649266分式: CHClNOS分量: 752.21作靶点: Bacterial作通路: Anti-infection储存式: -20C, stored under nitrogen* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 50 mg/mL (66.47 mM; Need ultraso

2、nic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.3294 mL 6.6471 mL 13.2942 mL5 mM 0.2659 mL 1.3294 mL 2.6588 mL10 mM 0.1329 mL 0.6647 mL 1.3294 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现现配，即刻使。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条

3、件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (3.66 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (3.66 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (3.66 m

4、M); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Cefiderocol种新型铁载体头孢 素，对有氧兰 性细 种类具有强效谱的活性。IC50 & Target MIC50: 1体外研究 Cefiderocol (CFDC; S-649266), a novel parenteral siderophore cephalosporin conjugated with a catecholmoiety, has a characteristic antibacteria

5、l spectrum with a potent activity against a broad range of aerobicGram-negative bacterial species, including carbapenem-resistant strains of Enterobacteriaceae andnonfermenting bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii. Cefiderocol hasaffinity mainly for penicillin-binding

6、protein 3 (PBP3) of Enterobacteriaceae and nonfermenting bacteriasimilar to that of ceftazidime. A deficiency of the iron transporter PiuA in P. aeruginosa or both CirA and Fiu inEscherichia coli can cause 16-fold increases in cefiderocol MICs, suggesting that these iron transporterscontribute to th

7、e permeation of cefiderocol across the outer membrane. The deficiency of OmpK35/36 inKlebsiella pneumoniae and the overproduction of efflux pump MexA-MexB-OprM in P. aeruginosa show nosignificant impact on the activity of cefiderocol 1.PROTOCOLCell Assay 1 For the determination of cefiderocol MIC, i

8、ron-depleted cation-adjusted Mueller-Hinton broth (ID-CAMHB) isprepared, except for the cases that are required to determine MICs under specific conditions. The qualitycontrol MIC ranges of cefiderocol are 0.06 to 0.5 g/mL for both E. coli ATCC 25922 and P. aeruginosaATCC 27853. For anaerobic bacter

9、ia, brucella agar supplemented with hemin, vitamin K1, and laked sheepblood is used. For recombinant strains, test medium is supplemented with 10 g/mL of gentamicin and/or 0.1mM IPTG (isopropyl-d-thiogalactopyranoside) when required 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ito A, et al. In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria.Antimicrob Agents Chemother. 2017 Dec 21;62(1).McePdfHeightCaution: Product has not been fully validate