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Cefoperazone

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Chemical Structure| 62893-19-0 同义名 : -
CAS号 : 62893-19-0
货号 : A194605
分子式 : C25H27N9O8S2
纯度 : 98%
分子量 : 645.667
MDL号 : MFCD00865067
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(162.62 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

IP 2% DMSO+2% Tween80+30% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 54 mg/mL suspension

生物活性
描述 Cefoperazone is a third‐generation cephalosporin and is one of a small number of cephalosporins that are effective in treating Pseudomonas bacterial infections (MIC50 25 μg/mL). The hydrolysis product of cefoperazone was noncovalently bound in the active site of PBP3. This may be important in the design of new noncovalent PBP3 inhibitors[3]. After intramuscular injection of 2 g of cefoperazone, the mean peak serum level was 111 microgram/ml at 1.5 hours. At 12 hours after dosing, mean serum levels were still 2 to 4 microgram/ml. Cefoperazone was 90% bound to serum proteins[4]. Both the inhibitory potency of the cephalosporins for Mrp2-mediated (multidrug resistance-associated protein) transport and the uptake of cephalosporins by Mrp2-expressing vesicles were molecular weight-dependent[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
NCT03003273 Neutropenia, Febrile ... 展开 >> Pediatric Cancer 收起 << Phase 3 Recruiting December 2018 India ... 展开 >> Department of Medical Oncology, AIIMS Recruiting New Delhi, India, 110029 Contact: Sameer Bakhshi, MD    011-29575237    sambakh@hotmail.com 收起 <<
NCT01601093 Respiratory Tract Infections ... 展开 >> Urinary Tract Infections 收起 << Phase 2 Unknown November 2013 China, Jiangsu ... 展开 >> the First Affiliated Hospital With Medical University Recruiting Nanjing, Jiangsu, China Contact: hong wh wang, doctor    025-83714511 ext 6360       Sub-Investigator: mao hm huang, doctor 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.55mL

0.31mL

0.15mL

7.74mL

1.55mL

0.77mL

15.49mL

3.10mL

1.55mL

参考文献

[1]Kato Y, Takahara S, et al. Involvement of multidrug resistance-associated protein 2 (Abcc2) in molecular weight-dependent biliary excretion of beta-lactam antibiotics. Drug Metab Dispos. 2008 Jun;36(6):1088-96.

[2]Craig WA, Gerber AU. Pharmacokinetics of cefoperazone: a review. Drugs. 1981;22 Suppl 1:35-45.

[3]Ren J, Nettleship JE, Males A, Stuart DI, Owens RJ. Crystal structures of penicillin-binding protein 3 in complexes with azlocillin and cefoperazone in both acylated and deacylated forms. FEBS Lett. 2016 Jan;590(2):288-97.

[4]Craig WA, Gerber AU. Pharmacokinetics of cefoperazone: a review. Drugs. 1981;22 Suppl 1:35-45.

[5]Kato Y, Takahara S, Kato S, Kubo Y, Sai Y, Tamai I, Yabuuchi H, Tsuji A. Involvement of multidrug resistance-associated protein 2 (Abcc2) in molecular weight-dependent biliary excretion of beta-lactam antibiotics. Drug Metab Dispos. 2008 Jun;36(6):1088-96.