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作靶點(diǎn): Bacterial作通路: Anti-infection儲存式: -20C, stored under nitrogen* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (66.47 mM; Need ultraso

2、nic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條

3、件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (3.66 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (3.66 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (3.66 m

4、M); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Cefiderocol種新型鐵載體頭孢 素，對有氧蘭 性細(xì) 種類具有強(qiáng)效譜的活性。IC50 & Target MIC50: 1體外研究 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