Cephacetrile
(Synonyms: 头孢乙氰,Cephacetrile; Cephacetril) 目录号 : GC49593
A cephalosporin antibiotic
Cas No.:10206-21-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cephacetrile is a cephalosporin antibiotic.1 It is active against numerous Gram-positive and Gram-negative bacteria, including clinical isolates of S. aureus, S. epidermidis, S. pyogenes, E. coli, and Klebsiella (MICs = 0.64, 0.64, 0.16, 6.25 and 3.12 µg/ml, respectively). Cephacetrile (30 µg/disc) is also active against veterinary isolates of S. aureus from bovine mastitis.2 Formulations containing cephacetrile have been used in the treatment of bovine mastitis.
1.Neu, H.C., and Winshell, E.B.In vitro evaluation of cephacetrile, a new cephalosporin antibioticJ. Antibiot. (Tokyo)25(7)400-404(1972) 2.Costa, E.O., Benites, N.R., Guerra, J.L., et al.Antimicrobial susceptibility of Staphylococcus spp. isolated from mammary parenchymas of slaughtered dairy cowsJ. Vet. Med. B Infect. Dis. Vet. Public Health47(2)99-103(2000)
| Cas No. | 10206-21-0 | SDF | Download SDF |
| 别名 | 头孢乙氰,Cephacetrile; Cephacetril | ||
| Canonical SMILES | O=C(OCC(CS[C@]1([H])[C@@H]2NC(CC#N)=O)=C(C(O)=O)N1C2=O)C | ||
| 分子式 | C13H13N3O6S | 分子量 | 339.3 |
| 溶解度 | DMF: sparingly,DMSO: slightly soluble,Methanol: slightly soluble | 储存条件 | -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。 |
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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 | 2.9472 mL | 14.7362 mL | 29.4724 mL |
| 5 mM | 0.5894 mL | 2.9472 mL | 5.8945 mL |
| 10 mM | 0.2947 mL | 1.4736 mL | 2.9472 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。
Cephacetrile--application of pharmacokinetic data to dosage determination
Int J Clin Pharmacol Biopharm 1976 Apr;13(3):168-76.PMID:950258doi
This pharmacokinetic investigation was based on the determination of serum and urinary levles of Cephacetrile in 50 subjects given single intramuscular or intravenous doses of 0.5 or 1 gm of the antibiotic; 30 normal subjects, 10 patients with renal insufficiency, and 10 patients with chronic nephritis undergoing maintenance haemodialysis were included in this study. In normal subjects, mean serum half-life was 1.09 hours (Ke = 0.6337) after intramuscular injection of 0.5 gm Cephacetrile, 1.31 hours (Ke = 0.5276) after intramuscular injection of 1 gm, and 0.89 hours (Ke = 0.7806) after intravenous injection of 1 gm. Absorption half-life was 0.45 hours after intramuscular injection of 1 gm Cephacetrile. The urinary elimination of Cephacetrile over the first 6 hours after injection was on the average 72.7% of the administered dose. After intravenous injection of 1 gm of the antibiotic, the plasma clearance of Cephacetrile was 407 ml/min., and its renal clearance 313 ml/min. A linear correlation was found between the values of overall elimination rate constant (Ke) and creatinine clearance in the subjects under investigation (Ke = 0.0080 + 0.0061 ClCr). The established pharmacokinetic characteristics were used to calculate the maintenance and loading doses as well as the intervals between injections adjusted to creatinine clearance. These data constitute true dosage schemes adapted to the particular case of each patient according to his kidney function.
Double-blind comparison of Cephacetrile with cephalothin-cephaloridine
Antimicrob Agents Chemother 1974 Mar;5(3):247-54.PMID:4599121DOI:10.1128/AAC.5.3.247.
Under double-blind protocol, a controlled comparison was made between a new cephalosporin, Cephacetrile, and cephalothin or cephaloridine. The patient's primary physician determined the indications for treatment, and the dosage was uniform for each route of administration. Infecting strains of staphylococci and Proteus mirabilis had a lower median inhibitory concentration for cephalothin than Cephacetrile; the opposite was true for Escherichia coli and Klebsiella species. The average peak serum level 1 h after a dose of 2 g intravenously was 74.9 +/- 21 and 21.5 +/- 8.7 mug/ml for Cephacetrile and cephalothin, respectively; 6 h after the dose, the respective levels were 12.4 +/- 4.3 and 3.7 +/- 0.9 mug/ml. Renal clearances were similar and the plasma clearance was proportional to the serum levels. In the urine, the concentration of Cephacetrile was three times higher than that of cephalothin. Based on a percentage of therapeutic potential, success in the treatment of infections with susceptible organisms was 42 and 44% for the two different drug regimens. Initial bacterial resistance was found in about one-fifth of infections, and concomitant therapy with other drugs was practiced in one-half of the treatment courses. Intravenous use of Cephacetrile was discontinued prematurely more often than was use of cephalothin, suggesting less tolerance. Although there was no overt toxicity, more than 75% of patients on either regimen had some form of unwanted response to treatment, the most common being superinfection. From this limited but controlled experience, Cephacetrile can be considered comparable to cephalothin in antimicrobial treatment and overall side reactions.
Cephacetrile, a new cephalosporin: in vitro, pharmacological and clinical evaluation
Infection 1975;3(3):161-4.PMID:4377DOI:10.1007/BF01641340.
Cephacetrile, a parenteral cephalosporin, was evaluated for in vitro antibacterial activity, clinical pharmacology and effectiveness in the treatment of severe infections. The antibacterial activity against 187 isolates was determined by an agar-dilution technique. The MICs were 0.06 to 0.5 mug/ml for Group A Streptococcus, D. pneumoniae, and Staph. aureus, 4-6 mug/ml for E. coli and Klebsiella-Enterobacter 8-32 mug/ml for Pr. mirabilis and more than 500 mug/ml for Ps. aeruginosa. A few strains of Klebsiella and E. coli had MICs of more than 125 mcg/ml. Serum levels after 0.5 and 1 g of i.m. Cephacetrile were respectively 14.6 and 18.6 mug/ml after 1 hr, and 1.5 and 2.5 mug/ml after 6 hr. Serum levels after i.v. infusion of 0.5 and 1 g were respectively 16 and 25 mug/ml after 1 hr., and 1 and 2 mug/ml after 6 hr. Urine levels after 0.5 and 1 g i.m. Cephacetrile were respectively 500 and 650 mug/ml in the 0-3 hr period, and 250 and 300 mug/ml in the 3-6 hr period. Renal clearance was 166 +/- 5 ml/min/1.73 m2; renal excretion was about 20% of the dose 6 hr after i.m. injection. Cephacetrile was well tolerated when administered i.m. with lidocaine. Mild phlebitis occurred sometimes after i.v. infusions. The clinical response, evaluated in 36 patients with severe systemic, respiratory and urinary infections, was good in all but two cases.
Metabolic fate of Cephacetrile after parenteral administration in rats and rabbits
J Antibiot (Tokyo) 1976 Jan;29(1):81-90.PMID:931795DOI:10.7164/antibiotics.29.81.
1. The metabolic fate of 14C-cephacetrile was studied in rats and rabbits. The plasma level of intravenously injected Cephacetrile decreased with half-lives of 17 and 22 minutes in rats and rabbits respectively, this decline being associated with a rapid appearance of the active metabolite, desacetylcephacetrile. Intramuscularly injected Cephacetrile was rapidly absorbed by rats with a maximum plasma level at 20 minutes and a half-life of 16 minutes. Cephacetrile and desacetylcephacetrile did not enter erythrocytes. Cephacetrile was weakly bound to the plasma protein in the rat, rabbit and man. 2. Both in rats and rabbits, almost all of the injected radioactivity was excreted in the urine within 72 hours as the intact antibiotic and desacetylcephacetrile, only small amounts appearing in feces via bile. Neither the gamma-lactone of desacetyl-7-cyanacetamidocephalosporanic acid nor the violet-reddish pigment (CGP-695) produced from Cephacetrile were detectable in the plasma or urine of the animals. 3. In rats given the labeled antibiotic intravenously, the radioactivity was widely distributed with concentrations being high in the kidney, plasma and liver, and lowest in the brain. The radioactivity crossed the rat placenta and appeared in the fetus. Radioactivity in these tissues disappeared as the plasma level declined. 4. During daily intramuscular injection of 14C-cephacetrile to rat, no significant changes were observed in the peak level of the plasma radioactivity or in the half-lives. In addition, dosing of the labeled antibiotic for 7 days caused no increase in tissue levels of radioactivity.
High-performance liquid chromatographic determination of Cephacetrile
J Pharm Sci 1979 May;68(5):652-4.PMID:430511DOI:10.1002/jps.2600680539.
A rapid and accurate quantitative determination of Cephacetrile in finished bulk and dosage forms is reported. The high-performance liquid chromatographic method is free of interference by acetyl hydrolysis products and synthesis by-products. The assay can be performed in about 15 min, affording less than 0.7% coefficients of variation within and between days. The chromatographic results are in good agreement with the microbiological assay requested by the "Code of Federal Regulations" for certification of Cephacetrile sodium.