Cefozopran (SCE-2787)
(Synonyms: 头孢唑兰; SCE-2787) 目录号 : GC32236
头孢唑仑 (SCE-2787) (SCE-2787) 是一种半合成、非肠道、第四代头孢菌素。
Cas No.:113359-04-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefozopran(SCE 2787) is a fourth-generation cephalosporin.Target: AntibacterialCefozopran is a fourth-generation cephalosporin.
[1]. http://www.toku-e.com/Assets/MIC/Cefozopran%20hydrochloride.pdf
| Cas No. | 113359-04-9 | SDF | |
| 别名 | 头孢唑兰; SCE-2787 | ||
| Canonical SMILES | [O-]C(C(N1[C@@]2([H])[C@H](NC(/C(C3=NSC(N)=N3)=N\OC)=O)C1=O)=C(CS2)C[N+]4=C(C=CC=N5)N5C=C4)=O | ||
| 分子式 | C19H17N9O5S2 | 分子量 | 515.53 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9398 mL | 9.6988 mL | 19.3975 mL |
| 5 mM | 0.388 mL | 1.9398 mL | 3.8795 mL |
| 10 mM | 0.194 mL | 0.9699 mL | 1.9398 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Therapeutic effect of Cefozopran (SCE-2787), a new parenteral cephalosporin, against experimental infections in mice
Antimicrob Agents Chemother 1993 Jan;37(1):100-5.PMID:8431004DOI:10.1128/AAC.37.1.100.
The therapeutic effect of Cefozopran (SCE-2787), a new semisynthetic parenteral cephalosporin, against experimental infections in mice was examined. Cefozopran was more effective than cefpiramide and was as effective as ceftazidime and cefpirome against acute respiratory tract infections caused by Klebsiella pneumoniae DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, cefozopran was as effective as ceftazidime. The therapeutic effect of cefozopran against urinary tract infections caused by Pseudomonas aeruginosa P9 was superior to that of cefpirome and was equal to those of ceftazidime and cefclidin. In addition, cefozopran was more effective than ceftazidime and was as effective as flomoxef in a thigh muscle infection caused by methicillin-sensitive Staphylococcus aureus 308A-1. Against thigh muscle infections caused by methicillin-resistant S. aureus N133, cefozopran was the most effective agent. The potent therapeutic effect of cefozopran in those experimental infections in mice suggests that it would be effective against respiratory tract, urinary tract, and soft tissue infections caused by a variety of gram-positive and gram-negative bacteria in humans.
Comparative pharmacokinetics of SCE-2787 and related antibiotics in experimental animals
Antimicrob Agents Chemother 1992 Nov;36(11):2481-6.PMID:1489192DOI:10.1128/AAC.36.11.2481.
The pharmacokinetic properties of SCE-2787 administered intravenously at a dose of 20 mg/kg of body weight were studied with mice, rats, rabbits, dogs, and monkeys and were compared with those of ceftazidime, cefpirome, and cefclidin in mice and dogs. The area under the concentration-time curve for plasma after intravenous administration was the largest in monkeys, followed by those in dogs, rabbits, rats, and mice, in that order. The elimination half-life ranged from 0.2 to 0.3 h in mice and rats to 0.7 to 1.3 h in rabbits, dogs, and monkeys. In young dogs, the concentrations of SCE-2787 in plasma were somewhat lower than those in the mature dogs. SCE-2787 was distributed well to the tissues, and the highest concentration was found in the kidneys in all species tested; the distribution to the lungs, liver, and spleen was also good, but the concentrations in these tissues were lower than those in the plasma. The pharmacokinetic parameters and urinary excretion of SCE-2787 in mice and dogs were similar to those of ceftazidime, cefpirome, and cefclidin. The maximum concentrations in the cerebrospinal fluid of rats and rabbits were 0.8 and 1.3 micrograms/ml, and the relative percentages of the area under the concentration-time curve of SCE-2787 in the cerebrospinal fluid to that in the plasma were 4.6 and 6.4%, respectively. SCE-2787 was excreted mainly in the urine; the recovery rate ranged from 74% (rats) to 90% (dogs) of the dose. The biliary excretion of SCE-2787, however, was low, amounting to about 1.4% for mice and rats and less than 0.5% for rabbits and dogs. In rats, there was no accumulation in the tissues and no delay in urinary excretion upon multiple intravenous administration of 20 mg of SCE-2787 per kg once daily for 7 days. No active metabolites were found in the plasma or urine of animals given SCE-2787. The binding of SCE-2787 to serum protein in mice, rats, dogs, monkeys, and humans was less than 11% and similar to that of cefclidin.
Comparative pharmacokinetics and serum bactericidal activities of SCE-2787 and ceftazidime
Antimicrob Agents Chemother 1993 Sep;37(9):1835-41.PMID:8239592DOI:10.1128/AAC.37.9.1835.
Ceftazidime and the new SCE-2787 are parenteral cephalosporins with a broad antimicrobial spectrum. Pharmacokinetics, serum bactericidal activities, and side effects were investigated in a randomized crossover study. A total of 12 healthy volunteers received a 20-min infusion of 1.5 g of SCE-2787 or 2.0 g of ceftazidime. Serum and urine concentrations were determined by the bioassay method and by high-pressure liquid chromatography (HPLC). The mean (+/- standard deviation) drug concentrations in serum at the end of infusion of SCE-2787 and ceftazidime were 124.4 +/- 23.8 and 233.1 +/- 54.1 mg/liter, respectively. The urine recovery of SCE-2787 was 87.8% +/- 5.5% of dose in 24 h and for ceftazidime was 85.8% +/- 6.3% of dose in 24 h. Metabolites of SCE-2787 could not be detected by HPLC in serum or urine. Pharmacokinetic parameters were calculated both with a noncompartmental analysis and on the basis of an open two-compartment model (drugs are administered into and eliminated from a central compartment only. However, reversible drug distribution from the central space occurs simultaneously into one peripheral space). The area under the concentration time curve from 0 h to infinity of SCE-2787 was 197.9 +/- 25.4 mg.h/liter, and that of ceftazidime was 334.2 +/- 40.0 mg.h/liter. SCE-2787 had a mean terminal half-life in the elimination phase of 109.0 +/- 15.3 min, while that of ceftazidime was 99.0 +/- 13.4 min. The volume of distribution at steady state of SCE-2787 was 17.1 +/- 1.6 liters/70 kg, and that of ceftazidime was 122.9 +/- 1.3 liters/70 kg. The mean residence time of SCE-2787 was 136.4 +/- 15.4 min, and that of ceftazidime was 122.9 +/- 12.7 min. The renal clearance per. 1.73 m2 of SCE-2787 was 103.1 +/- 12.3 ml/min, and that of ceftazidime was 80.6 +/- 13.2 ml/min. The serum bactericidal activities were measured with the microdilution method of Stratton and Reller (L. B. Reller and C. W. Stratton, J. Infect. Dis. 136:196-204, 1977) against 40 clinically isolated strains. One hour after administration, we measured mean reciprocal bactericidal titers of SCE-2787 and ceftazidime, respectively, against Escherichia coli of 388 and 243, against Klebsiella pneumoniae of 395 and 138, against Pseudomonas aeruginosa of 13.0 and 12.7, and against Staphylococcus aureus of 32.2 and 4.0. No severe side effects were observed in this single drug administration.
In vitro and in vivo activities of SCE-2787, a new parenteral cephalosporin with a broad antibacterial spectrum
Antimicrob Agents Chemother 1992 Jul;36(7):1358-66.PMID:1510428DOI:10.1128/AAC.36.7.1358.
SCE-2787, a new cephalosporin having a condensed azolium moiety in the 3 position and an aminothiadiazolyl group in the 7 beta side chain, was evaluated for its in vitro and in vivo activities in comparison with those of ceftazidime, flomoxef, cefpirome, and E1040. Against methicillin-susceptible strains of Staphylococcus aureus and Staphylococcus epidermidis, SCE-2787 was more active than ceftazidime and E1040 and was as active as flomoxef and cefpirome, with MICs for 90% of strains tested (MIC90s) being 1.56 micrograms/ml or less. SCE-2787 was also active against Pseudomonas aeruginosa, for which the MIC90 was 6.25 micrograms/ml, which was lower than that of cefpirome and comparable to that of ceftazidime. SCE-2787 was marginally active against methicillin-resistant strains of staphylococci and Enterococcus faecalis, although its MIC90s were the lowest among those of the antibiotics tested. The activities of SCE-2787 against Streptococcus species, most members of the family Enterobacteriaceae, and Haemophilus influenzae exceeded those of ceftazidime and flomoxef and were comparable to those of cefpirome. Furthermore, MIC90s of SCE-2787 were significantly lower than those of ceftazidime for ceftazidime-resistant isolates of Citrobacter freundii and Enterobacter cloacae. SCE-2787 was resistant to hydrolysis by various types of beta-lactamases, including the Bush group 1 beta-lactamases, and had low affinities for these enzymes, with Km or Ki values of greater than 100 microM. The in vitro activity of SCE-2787 was reflected in its efficacy in mouse protection tests. Thus, SCE-2787 appears to be a promising cephalosporin that should be further evaluated in clinical trials.
In vitro activity of SCE-2787, a new cephalosporin with potent activity against Pseudomonas aeruginosa and members of the family Enterobacteriaceae
Antimicrob Agents Chemother 1994 Dec;38(12):2896-901.PMID:7695279DOI:10.1128/AAC.38.12.2896.
The in vitro activity of SCE-2787, 7-[(Z)-2-(5-amino-1,2,4-thiadiazol-3- yl)-2-methoxyiminoacetamido]-3-(1-imidazo[1,2-b]pyridazinium)methy l-3- cephem-4-carboxylate, was compared with those of ceftazidime, ceftriaxone, and imipenem against recent clinical isolates. SCE-2787 inhibited 50% of tested isolates of the family Enterobacteriaceae at < or = 0.25 micrograms/ml. SCE-2787 was equally active as or more active than ceftazidime and ceftriaxone against members of the Enterobacteriaceae, with the exception of Proteus vulgaris. The MIC of SCE-2787 at which 90% of the isolates of Pseudomonas aeruginosa were inhibited was 2 micrograms/ml, two- to fourfold lower than those of imipenem and ceftazidime, respectively. SCE-2787, like ceftazidime and imipenem, did not inhibit the majority of strains of Pseudomonas cepacia and Xanthomonas maltophilia. SCE-2787 inhibited beta-hemolytic streptococci at < or = 0.12 micrograms/ml, but it did not inhibit Enterococcus faecalis, Listeria monocytogenes, or the anaerobic species tested. Methicillin-resistant staphylococci required SCE-2787 MICs of > or = 16 micrograms/ml, whereas methicillin-susceptible staphylococci were inhibited by 2 micrograms/ml. No difference between the MICs and MBCs was noted, except for P. aeruginosa, for which there was a fourfold difference. SCE-2787 was active over a pH range of 6 to 8. The inoculum size of 10(5) to 10(7) CFU caused only a twofold change in the MIC for Escherichia coli and Staphylococcus aureus but a 4- to 16-fold change in Enterobacter cloacae and P. aeruginosa. beta-Lactamases from Bush groups 1, 2a, and 2b did not hydrolyze SCE-2787. There was significant hydrolysis of SCE-2787 by the beta-lactamases designated 2b', i.e., TEM-3, TEM-5, TEM-7, and TEM-9, and by the group 2d beta-lactamases. SCE-2787 had poor affinity for group 1 and group 2b enzymes and constitutively produced chromosomal beta-lactamases such as P-99 of Enterobacter cloacae and plasmid-mediated TEM-1 of E. coli. SCE-2787 has in vitro activity comparable to that of current parenteral cephalosporin and is more active against P. aeruginosa and S. aureus.