Tigemonam
(Synonyms: 替吉莫南) 目录号 : GC32360
Tigemonam是一种单菌霉素，可以抵抗革兰氏阴性需氧细菌病原体。
Cas No.:102507-71-1
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
Tigemonam is a monobactam, with potent activity against Gram-negative aerobic bacterial pathogens.
Tigemonam (0.25 mg/L) inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. The MIC90 for Enterobacter spp. is 16 mg/L and for Citrobacter 4 mg/L. Pseudomonas aeruginosa is resistant to tigemonam but susceptible to aztreonam. Tigemonam shows minimal inoculum dependence, between 102 and 106 cfu per spot[1].
Tigemonam shows potent activities against Escherichia coli SC 8294, E. coli SC 12199, Salmonella schottmulleri SC 3850, Proteus mirabilis SC 9575, Providencia rettgeri SC 8217, Klebsiella pneumoniae SC 12216, Serratia marcescens SC 9782, Enterobacter cloacae SC 11078, Haemophilus influenzae SC 10556, with ED50 of 1.4 mg/kg, 1.5 mg/kg, 0.7 mg/kg, 0.3 mg/kg, 0.2 mg/kg, 0.9 mg/kg, 0.5 mg/kg, 3.9 mg/kg and 1.8 mg/kg in mice[2].
[1]. Rylander M, et al. Comparative in-vitro activity of tigemonam, a new monobactam. J Antimicrob Chemother. 1988 Sep;22(3):307-13. [2]. Clark JM, et al. In vivo evaluation of tigemonam, a novel oral monobactam. Antimicrob Agents Chemother. 1987 Feb;31(2):226-9.
| Cas No. | 102507-71-1 | SDF | |
| 别名 | 替吉莫南 | ||
| Canonical SMILES | OC(CO/N=C(C1=CSC(N)=N1)\C(N[C@H]2C(C)(N(OS(=O)(O)=O)C2=O)C)=O)=O | ||
| 分子式 | C12H15N5O9S2 | 分子量 | 437.41 |
| 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。 |
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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 | 2.2862 mL | 11.4309 mL | 22.8618 mL |
| 5 mM | 0.4572 mL | 2.2862 mL | 4.5724 mL |
| 10 mM | 0.2286 mL | 1.1431 mL | 2.2862 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。
Tigemonam, an oral monobactam
Antimicrob Agents Chemother 1988 Jan;32(1):84-91.PMID:3279906DOI:10.1128/AAC.32.1.84.
Tigemonam is an orally administered monobactam. At less than or equal to 1 microgram/ml it inhibited the majority of strains of Escherichia coli, Klebsiella spp., Enterobacter aerogenes, Citrobacter diversus, Proteus spp., Providencia spp., Aeromonas hydrophila, Salmonella spp., Shigella spp., Serratia marcescens, and Yersinia enterocolitica. At less than or equal to 0.25 microgram/ml it inhibited Haemophilus spp., Neisseria spp., and Branhamella catarrhalis. It did not inhibit Pseudomonas spp. or Acinetobacter spp. Tigemonam was more active than cephalexin and amoxicillin-clavulanate and inhibited many members of the family Enterobacteriaceae resistant to trimethoprim-sulfamethoxazole and gentamicin. Some Enterobacter cloacae and Citrobacter freundii strains resistant to aminothiazole iminomethoxy cephalosporins and aztreonam were resistant to Tigemonam. The MIC for 90% of hemolytic streptococci of groups A, B, and C and for Streptococcus pneumoniae was 16 micrograms/ml, but the MIC for 90% of enterococci, Listeria spp., Bacteroides spp., and viridans group streptococci was greater than 64 micrograms/ml. Tigemonam was not hydrolyzed by the common plasmid beta-lactamases such as TEM-1 and SHV-1 or by the chromosomal beta-lactamases of Enterobacter, Morganella, Pseudomonas, and Bacteroides spp. Tigemonam inhibited beta-lactamases of E. cloacae and Pseudomonas aeruginosa but did not induce beta-lactamases. The growth medium had a minimal effect on the in vitro activity of Tigemonam, and there was a close agreement between the MICs and MBCs.
In vitro evaluation of Tigemonam, a novel oral monobactam
Antimicrob Agents Chemother 1987 Feb;31(2):219-25.PMID:3105448DOI:10.1128/AAC.31.2.219.
Tigemonam, a novel, orally administered monobactam, exhibited potent and specific activity in vitro against members of the family Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae. Its activity was variable to poor against gram-positive bacteria, Acinetobacter spp., Pseudomonas aeruginosa, and anaerobes. Within its spectrum of activity, Tigemonam was far superior to oral antibiotics currently available, including amoxicillin-clavulanic acid, cefaclor, and trimethoprim-sulfamethoxazole. In addition, Tigemonam was superior to cefuroxime, which is under development as an oral pro-drug, and more active than cefixime against several genera of the Enterobacteriaceae. The activity of Tigemonam against the enteric bacteria, Haemophilus species, and Neisseria species was, in general, comparable to that of the quinolone norfloxacin. The excellent activity of Tigemonam against beta-lactamase-producing bacteria reflected its marked stability to hydrolysis by isolated enzymes. The expanded spectrum of activity against gram-negative bacteria observed with Tigemonam thus extends oral beta-lactam coverage to include members of the Enterobacteriaceae that are intrinsically or enzymatically resistant to broad-spectrum penicillins and cephalosporins.
In vivo evaluation of Tigemonam, a novel oral monobactam
Antimicrob Agents Chemother 1987 Feb;31(2):226-9.PMID:3551830DOI:10.1128/AAC.31.2.226.
Tigemonam, a new monobactam with excellent activity against gram-negative bacteria, was evaluated for in vivo efficacy and absorption after oral administration to laboratory animals. Tigemonam is absorbed when administered orally to mice and dogs. In a variety of gram-negative systemic infections in mice, orally administered Tigemonam was efficacious in all infections studied. Comparison drugs such as amoxicillin, cephalexin, and cefaclor were less efficacious, especially in infections caused by beta-lactamase-producing organisms. In localized infections, Tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., Tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, Tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin. Tigemonam was well absorbed in laboratory animals and with its excellent gram-negative spectrum of activity should prove of value in oral antibiotic therapy in humans.
In vitro antimicrobial activity of Tigemonam, a new orally administered monobactam
Antimicrob Agents Chemother 1988 Mar;32(3):346-9.PMID:3259122DOI:10.1128/AAC.32.3.346.
At five geographically separate medical centers, over 6,000 clinical bacterial isolates were tested for their susceptibility to Tigemonam by the broth microdilution method. The antimicrobial spectrum of Tigemonam was similar to that of aztreonam, but with two differences. Aztreonam was more active against Pseudomonas spp., and Tigemonam was more active against some streptococci. Tigemonam was highly resistant to hydrolysis by the eight beta-lactamase enzymes tested. A significant (greater than a fourfold increase in the MICs of Tigemonam) inoculum effect occurred when 3 of 13 isolates were tested with inocula of 5 X 10(5) and 1 X 10(7) CFU/ml. Tigemonam was bactericidal for all but 1 of the 13 isolates. Of the four quality-control strains recommended by the National Committee for Clinical Laboratory Standards, only Escherichia coli ATCC 25922 provided on-scale results. The proposed MIC quality-control range of Tigemonam for E. coli ATCC 25922 is 0.13 to 0.5 micrograms/ml.
Comparative in-vitro activity of Tigemonam, a new monobactam
J Antimicrob Chemother 1988 Sep;22(3):307-13.PMID:3182428DOI:10.1093/jac/22.3.307.
The in-vitro activity against Gram-negative aerobic bacterial pathogens of a new oral monobactam, Tigemonam, was compared with those of amoxycillin/clavulanic acid, aztreonam, cefaclor, ceftazidime, cefuroxime, ciprofloxacin, co-trimoxazole and gentamicin, by an agar-dilution method. Tigemonam inhibited 90% of strains tested of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis at concentrations of 0.25 mg/l or below. The MIC90 for Enterobacter spp. was 16 mg/l and for Citrobacter 4 mg/l. Pseudomonas aeruginosa was resistant to Tigemonam but susceptible to aztreonam. In comparison with the other oral antibiotics tested, Tigemonam was generally more active. Tigemonam showed minimal inoculum dependence, between 10(2) and 10(6) cfu per spot. It is concluded that Tigemonam is a candidate for clinical trials in patients with infections caused by Gram-negative aerobes other than pseudomonas and acinetobacter.