Ceforanide
(Synonyms: 头孢雷特) 目录号 : GC60684
Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin.
Cas No.:60925-61-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin.
| Cas No. | 60925-61-3 | SDF | |
| 别名 | 头孢雷特 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC3=NN=NN3CC(O)=O)CS[C@]2([H])[C@H](NC(CC4=CC=CC=C4CN)=O)C1=O)O | ||
| 分子式 | C20H21N7O6S2 | 分子量 | 519.55 |
| 溶解度 | DMSO: 125 mg/mL (240.59 mM) | 储存条件 | -20°C, away from moisture |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9247 mL | 9.6237 mL | 19.2474 mL |
| 5 mM | 0.3849 mL | 1.9247 mL | 3.8495 mL |
| 10 mM | 0.1925 mL | 0.9624 mL | 1.9247 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。
Ceforanide: antibacterial activity, pharmacology, and clinical efficacy
Pharmacotherapy 1982 Nov-Dec;2(6):322-7.PMID:6762529DOI:10.1002/j.1875-9114.1982.tb03208.x.
Ceforanide is a new cephalosporin with a longer elimination half-life than any currently available cephalosporin. Its activity is very similar to that of cefamandole, a second-generation cephalosporin, except that Ceforanide is less active against most gram-positive organisms. Many coliforms, including Escherichia coli, Klebsiella, Enterobacter, and Proteus, are susceptible to Ceforanide, as are most strains of Salmonella, Shigella, Hemophilus, Citrobacter and Arizona species. However, most strains of Serratia marcescens and all Pseudomonas aeruginosa are resistant to this compound. Peak serum concentrations in excess of 100 micrograms/ml are achieved after a 1 g intravenous dose. The elimination half-life of Ceforanide is about 3 hrs in patients with normal renal function; this allows twice daily dosing for the majority of patients. As renal excretion amounts for 85-90% of drug elimination, the serum half-life increases to approximately 20 hours in anuric patients. Tissue penetration studies demonstrate inhibitory concentrations in cardiac tissue, bone, and joint fluid. Minor adverse effects have been reported after large doses of Ceforanide. Clinical trials indicate that Ceforanide is effective in the treatment of skin and soft tissue, pulmonary and urinary tract infections, bone and joint infections, and endocarditis. Ceforanide also has been shown to be as effective as cephalothin or cephaloridine when given prophylactically for vaginal hysterectomy.
Ceforanide kinetics
Clin Pharmacol Ther 1981 Sep;30(3):396-403.PMID:7273604doi
Pharmacologic studies of the semisynthetic cephalosporin Ceforanide were conducted in 29 cancer patients. Intravenous doses of 500 mg over 30 min every 6 hr to 10 patients induced mean peak serum concentrations between 44.7 and 51.5 micrograms/ml, while in 10 patients receiving 1 gm over 30 min every 12 hr mean peak serum concentrations varied from 73.4 to 91.8 micrograms/ml. Twelve hours after 1 gm of drug, mean serum concentrations varied between 5.6 and 6.5 micrograms/ml. After a 500-mg loading dose, continuous infusion of 500 mg every 4 hr, 10 patients maintained serum concentrations above 34.2 micrograms/ml for 7 or 8 days. Most of the drug was excreted in the urine in the initial 6 hr after administration and mean urinary concentration of 1,315 micrograms/ml were obtained during this time. Serum half-life ranged between 2.2 and 2.9 hr on all schedules and therefore wa longer than that of other cephalosporins. No serious toxicity was noted. The relatively broad spectrum of activity in addition to the long half-life suggests clinical utility for this drug.
Ceforanide. A review of its antibacterial activity, pharmacokinetic properties and clinical efficacy
Drugs 1987 Oct;34(4):411-37.PMID:3315624DOI:10.2165/00003495-198734040-00001.
Ceforanide is a 'second generation' cephalosporin administered intravenously or intramuscularly. It is similar to cefamandole and cefonicid in its in vitro superiority to 'first generation' cephalosporins against several species of Enterobacteriaceae as well as its activity against Haemophilus influenzae, including beta-lactamase-producing strains. Its activity against Staphylococcus aureus is less than that of cefamandole, cefuroxime and first generation cephalosporins. The in vitro activity against Neisseria gonorrhoeae is excellent. Pseudomonas, Acinetobacter and Serratia species, and Bacteroides fragilis are resistant, as are many strains of Proteus and Providencia species. The elimination half-life is relatively long, although shorter than that of cefonicid, and in most clinical trials Ceforanide has been administered twice daily. It appeared to be comparable in therapeutic efficacy to procaine penicillin and cephazolin in the treatment of patients with community-acquired pneumonia, to cephazolin in the treatment of skin and soft tissue infections due to S. aureus or beta-haemolytic streptococci and to cefapirin in S. aureus endocarditis in parenteral drug abusers. Also, it was comparable in efficacy to cephalothin in the prophylaxis of infection in patients undergoing open heart surgery or vaginal hysterectomy, and to cephazolin in patients undergoing cholecystectomy. Thus, Ceforanide is an alternative to first and certain other second generation cephalosporins in several important therapeutic and prophylactic situations. It has no advantage over other cephalosporins with regard to spectrum of antibacterial activity, but has a longer half-life than other second generation cephalosporins, except cefonicid, and can be administered according to a twice daily dosage schedule.
Pharmacokinetics of Ceforanide
Antimicrob Agents Chemother 1982 Feb;21(2):323-6.PMID:7073268DOI:10.1128/AAC.21.2.323.
The pharmacokinetic of Ceforanide, a new parenteral cephalosporin antibiotic, were examined at intravenous and intramuscular doses of 250, 500, and 1,000 mg in healthy male volunteers. Over the above dosing range, Ceforanide pharmacokinetics were essentially linear, with plasma clearances varying from 2.2 to 2.5 liters/h. The best present overall estimate of the drug's half-life was 2.9 h. Intramuscular Ceforanide was 100% bioavailable, Peak intravenous serum levels were 39, 71, and 135 micrograms/ml at the end of 30-min infusions of 250, 500, and 1,000 mg; after intramuscular injections of 250, 500, and 1,000 mg, the respective peak serum levels were 21, 38, and 69 micrograms/ml. From 80 to 85% of the above doses were eliminated as unchanged.
Ceforanide kinetics in renal insufficiency
Clin Pharmacol Ther 1981 Oct;30(4):468-74.PMID:7285481DOI:10.1038/clpt.1981.190.
Ceforanide (500 mg) was infused intravenously over 30 min into six normal subjects, 10 nondialysis patients with renal insufficiency, and six hemodialysis patients. Dialysis patients received two Ceforanide infusions, one immediately before dialysis and another during an interdialysis period. Sequential plasma samples over 24 to 72 hr were assayed for Ceforanide. Peak Ceforanide levels (mean = 69 +/- 12 micrograms/ml) and volumes of distribution did not vary with creatinine clearance (Clcr, ml/min/1.73 m2) and both plasma clearance and renal clearance decreased linearly as Clcr decreased. Mean nonrenal clearance (4.6 +/- 1.8 ml/min/1.73 m2) did not vary with Clcr. Mean half-life was 3 hr in the normal subjects, increasing to approximately 25 hr in patients with severe renal insufficiency. Hemodialysis resulted in a removal of approximately 21% of the dose of Ceforanide. Dosing recommendations for patients with renal insufficiency are provided.