Cefpiramide sodium (SM-1652)
(Synonyms: 头孢匹胺钠; SM-1652; Wy-44635) 目录号 : GC33961
Cefpiramide sodium (CPMS, SM-1652,wy-44635) is an anionic β-lactam antibiotic. It exhibits antibacterial activity against gram-positive and gram-negative bacteria, in particular, to Pseudomonas aeruginosa, which can result in achronic life-threatening infection in the lungs of cystic fibrosis patients.
Cas No.:74849-93-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefpiramide sodium (CPMS, SM-1652,wy-44635) is an anionic β-lactam antibiotic. It exhibits antibacterial activity against gram-positive and gram-negative bacteria, in particular, to Pseudomonas aeruginosa, which can result in achronic life-threatening infection in the lungs of cystic fibrosis patients.
[1] Sun Q, et al. J Drug Target. 2011;19(1):49-55.
| Cas No. | 74849-93-7 | SDF | |
| 别名 | 头孢匹胺钠; SM-1652; Wy-44635 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC3=NN=NN3C)CS[C@]2([H])[C@H](NC([C@H](NC(C4=C(O)C=C(C)N=C4)=O)C5=CC=C(O)C=C5)=O)C1=O)O.[Na] | ||
| 分子式 | C25H24N8NaO7S2 | 分子量 | 635.63 |
| 溶解度 | DMSO : ≥ 39 mg/mL (61.36 mM) | 储存条件 | 4°C, protect from light ,unstable in solution, ready to use. |
| 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 | 1.5732 mL | 7.8662 mL | 15.7324 mL |
| 5 mM | 0.3146 mL | 1.5732 mL | 3.1465 mL |
| 10 mM | 0.1573 mL | 0.7866 mL | 1.5732 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。
Pharmacokinetics of cefpiramide (SM-1652) in humans
Antimicrob Agents Chemother 1984 Feb;25(2):221-5.PMID:6712202DOI:10.1128/AAC.25.2.221.
The pharmacokinetics of cefpiramide (SM-1652) were studied after the intravenous administration of single or multiple doses to 21 healthy volunteers. The cefpiramide concentration in plasma at time zero after a bolus intravenous injection of 500 or 1,000 mg was 152 or 303 micrograms/ml, respectively. The maximum cefpiramide level in plasma at the end of a 1-h infusion of 1,000 or 2,000 mg was 166 or 317 micrograms/ml, respectively. The mean plasma half-life of cefpiramide in 15 subjects who received a single dose of 500 or 1,000 mg was 4.44 h. There was no evidence of drug accumulation in plasma when 500 or 1,000 mg of cefpiramide was administered 11 times at 12-h intervals. Urinary excretion of cefpiramide over a 24-h period was ca. 22.5%, regardless of the intravenous administration technique and the dosage. Fecal recoveries of cefpiramide varied from 0 to 36.9% in different subjects.
Renal tubular mechanisms for excretion of cefpiramide (SM-1652) in association with its long-lasting pharmacokinetic properties
J Pharmacobiodyn 1988 Feb;11(2):67-73.PMID:3379566DOI:10.1248/bpb1978.11.67.
To investigate possible mechanisms for the long-lasting pharmacokinetic properties of cefpiramide, pharmacokinetic and renal clearance studies were carried out using rabbits. Cefazolin was employed as a reference compound. In pharmacokinetic studies, the plasma half-life (t1/2 beta) for cefpiramide was 2.7 times as long as that for cefazolin. The total body clearance (ClT) and renal clearance (ClR) for cefazolin were approximately 2.3 times larger than those for cefpiramide. In renal clearance studies, the clearance by glomerular filtration (Clf) for cefpiramide exceeded Clf for cefazolin by 2.5 times, because of lower plasma protein binding of cefpiramide. In contrast, the clearance by tubular secretion (Cls) for cefpiramide was one-fifth as small as Cls for cefazolin. The overall renal clearance (Clr) for cefazolin was 3.6 times as large as Clr for cefpiramide, being in good agreement with the cefazolin/cefpiramide ratios of ClT and ClR. Therefore, the long-lasting pharmacokinetic properties of cefpiramide was suggested to be due to the fact that cefpiramide undergoes renal tubular secretion to less extent.
Antibacterial activities of SM-1652 compared with those of other broad-spectrum cephalosporins
Antimicrob Agents Chemother 1982 Nov;22(5):721-7.PMID:6983860DOI:10.1128/AAC.22.5.721.
The in vitro and in vivo activities of SM-1652 were compared with those of other cephalosporins. SM-1652 possessed a wide antibacterial spectrum which included activity against Pseudomonas aeruginosa. It also exhibited potent antibacterial activities against gram-positive cocci and clinical isolates of glucose nonfermentative bacteria. Most notably, its activity against glucose nonfermentative bacteria was the highest of all of the drugs tested. The bactericidal activity of SM-1652 was compared with that of cefoperazone. The difference between the minimum bactericidal concentration and the minimum inhibitory concentration of SM-1652 was actually smaller than that of cefoperazone for Escherichia coli and clinical isolates of indole-positive Proteus spp. SM-1652 was stable for most cephalosporinases but was hydrolyzed to some extent by penicillinases. The in vivo therapeutic effect of SM-1652 against infections in mice was better than those of cefazolin and cefoxitin. The in vivo antipseudomonal activity of SM-1652 was second to that of cefsulodin.
In vitro activity of cefpiramide (SM-1652) against gram-negative bacilli
Diagn Microbiol Infect Dis 1986 Jan;4(1):77-81.PMID:3943292DOI:10.1016/0732-8893(86)90060-x.
The susceptibilities of 317 gram-negative bacilli to cefpiramide, cefotaxime, and piperacillin were determined by standardized microdilution and disk diffusion tests. Cefpiramide and piperacillin were more consistently active against nonfermenters than against Enterobacteriaceae, whereas cefotaxime was more active against Enterobacteriaceae. Inhibitory zone diameters of approximately 75-micrograms cefpiramide disks correlated well with minimal inhibitory concentrations (r = 0.85); breakpoints for defining susceptibility and resistance were recommended.
Pharmacokinetics of the cephalosporin SM-1652 in mice, rats, rabbits, dogs, and rhesus monkeys
Antimicrob Agents Chemother 1982 Aug;22(2):213-7.PMID:6927282DOI:10.1128/AAC.22.2.213.
The pharmacokinetics of SM-1652 were studied in mice, rats, rabbits, dogs, and rhesus monkeys. The plasma half-lives of SM-1652, administered intravenously at a dose of 20 mg/kg, were 11.0 min in mice, 26.0 min in rats, 65.8 min in rabbits, 72.6 min in dogs, and 150.9 min in monkeys. The 24-h urinary excretion of SM-1652 was 30 to 35% of the dose in mice and rats, 70 to 75% in rabbits and dogs, and 45% in monkeys. Biliary excretion of the antibiotic over a 24-h period was 60 and 19% in rats and rabbits, respectively; it was 19% in dogs over a 9-h period after SM-1652 administration. Approximately 95% of the intravenous dose of SM-1652 was recovered as the unchanged form in the urine and bile of rats and rabbits. The binding of SM-1652 to serum protein was 44.0% in mice, 46.0% in rats, 90.4% in rabbits, 93.2% in monkeys, 30.0% in dogs, and 96.3% in humans.