Cefotetan
(Synonyms: 头孢替坦) 目录号 : GC38032
A cephamycin antibiotic
Cas No.:69712-56-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefotetan is a cephamycin antibiotic that is active against both Gram-positive and Gram-negative bacteria including isolates of E. coli, S. aureus, K. pneumoniae, and P. maltophilia (MICs = 0.03-32 mg/ml).1 It reduces mortality by 50% in a rabbit model of fecal peritonitis when administered at a dose of 25 mg/kg twice daily.2 Formulations containing cefotetan have been used in the treatment of various bacterial infections.
1.Daschner, F.D., Goerke, C., Bassler, M., et al.In vitro comparison of cefotetan with five other cephalosporins against nosocomial pathogensChemotherapy28(5)351-354(1982) 2.Ablan, C.J., Olen, R.N., Dobrin, P.B., et al.Efficacy of intraperitoneal antibiotics in the treatment of severe fecal peritonitisAm. J. Surg.162(5)453-456(1991)
| Cas No. | 69712-56-7 | SDF | |
| 别名 | 头孢替坦 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC3=NN=NN3C)CS[C@]2([H])[C@](OC)(NC(C(S/4)SC4=C(C(O)=O)/C(N)=O)=O)C1=O)O | ||
| 分子式 | C17H17N7O8S4 | 分子量 | 575.62 |
| 溶解度 | DMSO: 250 mg/mL (434.31 mM) | 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。 |
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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 | 1.7373 mL | 8.6863 mL | 17.3726 mL |
| 5 mM | 0.3475 mL | 1.7373 mL | 3.4745 mL |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7373 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。
Cefotetan-bound human RKIP involves in Ras/Raf1/MEK/ERK signaling pathway
Acta Biochim Biophys Sin (Shanghai) 2022 Dec 25;54(12):1917-1923.PMID:36789691DOI:10.3724/abbs.2022188.
Cefotetan is widely used to treat bacterial infections in the clinic owing to its broad spectrum of antibacterial activity. In the present study, we demonstrate that Cefotetan can bind to the conserved ligand-binding pocket of human Raf1 kinase inhibitory protein (hRKIP), which acts as a negative regulator of the Ras/Raf1/MEK/ERK signaling pathway. The cefotetan-bound hRKIP adopts a rigid structure with insufficient space for binding Raf1 kinase, thereby reliving the inhibitory activity of hRKIP in the Ras/Raf1/MEK/ERK signaling pathway and enhancing the phosphorylation level of ERK. Both NMR titration and molecular docking approaches show that several residues (P74, Y81, W84, P111, P112, K113, S142, G143, D144, W173, P178, Y181 and L184) play crucial roles in hRKIP binding Cefotetan. NMR dynamics analysis reveals that the binding of Cefotetan with hRKIP promotes ps-ns internal motion but reduces μs-ms conformational exchange for residues in the cefotetan-binding pocket of hRKIP. Our results not only disclose the structural basis of Cefotetan upregulating the Ras/Raf1/MEK/ERK signaling pathway but also benefit developing novel drugs against diseases caused by the impaired Ras/Raf1/MEK/ERK pathway.
Cefotetan: a review of the microbiologic properties and antimicrobial spectrum
Am J Surg 1988 May 31;155(5A):16-23.PMID:3287964DOI:10.1016/s0002-9610(88)80207-1.
Cefotetan (formerly ICI 156834 and YM09330) is a 7-methoxy cephalosporin possessing some advantageous antimicrobial spectrum, safety, and pharmacokinetic characteristics compared with other so-called second-generation cephalosporins. The published literature was reviewed and the Cefotetan quantitative susceptibility testing data from nearly 31,000 isolates was tabulated. Against 15,769 enteric bacilli, Cefotetan was observed to have a potency and spectrum more closely resembling a third-generation cephalosporin and markedly superior to cefoxitin. The mean of all MIC 90s reported for the Enterobacteriaceae ranged from 0.06 to 13 micrograms/ml except for citrobacter species, E. cloacae, Enterobacter species, and C. freundii. The mean MIC 50 for all 22 recorded species was in the susceptible range. Cefotetan was very effective against B. catarrhalis, H. influenzae, and pathogenic Neisseria species. However, Cefotetan and cefoxitin were not active against Pseudomonas species, Acinetobacter species, and some rarely isolated species. Cefotetan was moderately active against the staphylococci (mean MIC 50, 7.6 to 26 micrograms/ml) and streptococci (mean MIC 50, 0.9 to 6.6 micrograms/ml). The coagulase-negative staphylococcus species generally had higher Cefotetan and cefoxitin minimum inhibitory concentrations compared with the S. aureus isolates. Oxacillin-resistant staphylococci were resistant to Cefotetan. The enterococci, JK group diphtheroids, Corynebacterium species, and L. monocytogenes isolates were resistant. A review of 4,751 strict anaerobes showed Cefotetan to have a very comparable activity and spectrum to cefoxitin. The 1,291 B. fragilis strains had a mean MIC 50 and MIC 90 of 5.4 and 23 micrograms/ml, respectively. These values were slightly superior to cefoxitin when tested in parallel. More elevated minimum inhibitory concentrations were observed for other B. fragilis group species for cefoxitin and Cefotetan. The mean Cefotetan MIC 90 for all other anaerobic bacteria except the Eubacterium species and Lactobacillus species predict favorable clinical efficacy. The beta-lactamase stability of Cefotetan is very similar to that of other 7-methoxy cephalosporins. Cefotetan also inhibits Type Ia cephalosporinases with high enzyme affinity and is an inducer of these beta-lactamases, although Cefotetan is not rapidly hydrolyzed. Synergy between Cefotetan and numerous other antibiotics has been reported, but antagonism has also been occasionally observed.
Cefotetan. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use
Drugs 1985 Nov;30(5):382-426.PMID:3905336DOI:10.2165/00003495-198530050-00002.
Cefotetan is a new semisynthetic cephamycin antibiotic administered intravenously or intramuscularly. It has a broad spectrum of activity against Gram-negative aerobic and most clinically important Gram-positive and anaerobic bacteria, and is generally more active against Gram-negative bacteria than the 'first and second generation' agents. Cefotetan is particularly active against Enterobacteriaceae but has little activity against Pseudomonas aeruginosa. An extended plasma elimination half-life of about 3.5 hours, and relatively high achievable serum and tissue levels, enables Cefotetan to be administered on a twice daily basis in the treatment of mild to severe infections. Cefotetan has shown good clinical efficacy in intra-abdominal, obstetric and gynaecological infections, postoperative wound infections, and infections in immunocompromised patients - all of which are often complicated due to their polymicrobial nature or by the presence of anaerobic pathogens. A satisfactory clinical response is achieved in over 90% of paediatric patients with acute otorhinolaryngological infections, whereas in the treatment of chronic disease, as with other agents, the efficacy is dramatically reduced. Like other cephalosporins, Cefotetan is effective in treating patients with complicated urinary tract infections and lower respiratory tract infections. Its efficacy in urinary tract infections is at least as good as cefoxitin, although in this and some other clinical areas its activity relative to that of other cephamycins and cephalosporins remains to be assessed. Thus, with its convenient twice daily dosage schedule, Cefotetan would appear to be a useful addition to a rapidly expanding group of antibacterial agents.
Cefotetan-induced anaphylaxis
Am J Obstet Gynecol 1988 Jul;159(1):125-6.PMID:3164980DOI:10.1016/0002-9378(88)90506-6.
Three cases of anaphylactic reactions associated with the use of intravenous Cefotetan as surgical prophylaxis for cesarean section (two cases) and transabdominal hysterectomy (one case) are presented. Comprehensive review of these cases revealed no evidence of lot-specific association, drug-drug interaction, or methodologic variance. During the 4-month interval that Cefotetan was selectively used for surgical prophylaxis at our hospital, we observed a 1.4% incidence of anaphylactic hypersensitivity reactions associated with its use.
Clinical pharmacokinetics of Cefotetan
Clin Pharmacokinet 1994 Apr;26(4):248-58.PMID:8013159DOI:10.2165/00003088-199426040-00002.
Cefotetan is a 7-alpha-methoxy beta-lactam. A long serum half-life and resistance to beta-lactamase hydrolysis have made Cefotetan an attractive chemotherapeutic agent, and the results of clinical trials worldwide have demonstrated its efficacy in a wide variety of clinical situations. Cefotetan can be administered intravenously (bolus or infusion) or intramuscularly with lidocaine (lignocaine) 0.5%. Mean peak plasma concentrations are almost linearly related to dose. The volume of distribution is between 8 and 13L and is not different from other cephalosporins. No accumulation is seen after repeated doses and no metabolite has been detected in either plasma or urine. Total body clearance is 1.8 to 2.9 L/h. Renal clearance accounts for about 64 to 84% of a dose, and 75% of a dose is excreted in the urine within 24 hours. The plasma elimination half-life is between 3 and 4 hours after intravenous and intramuscular doses. Half-life is considerably prolonged in patients with renal impairment (up to 10 hours). Cefotetan concentrations are likely to be active against susceptible bacteria in most tissues and body fluids. Breast milk and cerebrospinal fluid concentrations are low. The recommended dosage is 1g every 12 hours, increasing to 2g in severe infections and 3g in life-threatening infections. In surgical prophylaxis, a single dose of 2g is given with the induction of anaesthesia; an additional dose of 2g may be administered 12 hours later. In children over 6 months, the recommended dosage is 30 mg/kg given 12-hourly. In patients with a creatinine clearance of 10 to 40 ml/min (0.6 to 2.4 L/h), the dose is halved or the dosage interval is doubled. When creatinine clearance is less than 10 ml/min (0.6 L/h), the dose is quartered or the dosage interval quadrupled.