Bicyclomycin Benzoate
(Synonyms: 双环霉素苯酸盐,FR2054) 目录号 : GC14866
An antibiotic against Gram-negative bacteria
Cas No.:37134-40-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Bicyclomycin benzoate is a novel antibiotic produced by S. sapporonensi [1]. Bicyclomycin shows an inhibitory effect on Gram-negative bacteria, such as E. coli, Klebsiella, Shigella, Salmonella, Citrobacter, E. cloacae, and the pathogenic group of Neisseria [2]. Bicyclomycin benzoate is inactive against Proteus, P. aeruginosa, and Gram-positive bacteria [1,2].
In vitro: The MIG of bicyclomycin for E.coli NIHJ JC-2 was 25-50 μg/ml. Bicyclomycin (25-50 μg/ml) completely inhibited formation of visible colonies or turbidity of this organism on agar plates, in nutrient broth, and in heart infusion broth [2]. Bicyclomycin inhibited ATPase activity in the presence of poly(dC) and ribo(C)10. The approximate IC50 value for inhibition of transcription termination at Rho-dependent sites was 5 μM. The inhibitory effect of bicyclomycin on Rho-dependent transcripts was accompanied by the appearance of a new set of transcripts. In the presence of poly(dC), bicyclomycin reversibly inhibited the ribo(C)10-stimulated ATPase activity. The extrapolated Ki for bicyclomycin was 2.8 μM without ribo(C)10, which was increased to 26 μM in the presence of ribo(C)10 [3].
In vivo: Bicyclomycin showed therapeutic activity for infections with several strains of E. coli which were resistant to the control antibiotics. The ED50 of bicyclomycin for infection with GP-resistant E.coli 312 was 3.05 (1.47-7.66) mg/mouse [2].
References:
[1] Miyoshi, T. ,Miyairi, N.,Aoki, H., et al. Bicyclomycin, a new antibiotic. I. Taxonomy, isolation and characterization. J.Antibiot.(Tokyo) 25(10), 569-575(1972).
[2] Nishida, M. ,Mine, Y.,Matsubara, T., et al. Bicyclomycin, a new antibiotic. III. In vitro and in vivo antimicrobial activity. J.Antibiot.(Tokyo) 25(10), 582-593(1972).
[3] Magyar A, Zhang X, Kohn H, et al. The antibiotic bicyclomycin affects the secondary RNA binding site of Escherichia coli transcription termination factor Rho[J]. Journal of Biological Chemistry, 1996, 271(41): 25369-25374.
Kinase experiment: | ATPase activity assays are carried out with rho (100 ng) except that either bicyclomycin (0–60 μM) or dihydrobicyclomycin (0–90 μM) is added to the reaction solution. The samples are preheated to 32°C (2.5 min), and the reaction is initiated by the addition of ATP (9.1–100 μM) and [g-32P]ATP (0.5mCi) to the side of the tube, briefly vortexed, centrifuged (2 s), and returns to the water bath. Aliquots (1 mL) are removed at five time points (15, 30, 45, 60, and 75 s), and spotted on Baker-Flex cellulosePEI TLC plates. The rates of reaction are determined by measuring the relative amount of radiolabeled inorganic phosphate and ATP and then plotting the amount of ATP hydrolyzed versus time. The initial rates for each ATP concentration plus or minus inhibitors are plotted as double reciprocal plots[3]. |
Animal experiment: | Rats: A total of 25 SD male rats receives intramuscular administration of bicyclomycin at a single dose of 50mg/kg. Blood samples are taken by heart-puncture from 5 rats each at 0.5, 1, 2, 3, and 5 hours after the administration[4]. Mice: A total of 40 ICR male mice receives intramuscular administration of bicyclomycin at a single dose of 50mg/kg. Eight mice each are bled at 5, 10, 20, 30 and 60 minutes after administration by heart-puncture with heparin[4]. Rabbits: Five rabbits and 5 dogs are given bicyclomycin intramuscularly at a single dose of 50 mg/kg and blood samples are withdrawn from these animals at similar intervals. The samples are allowed to clot and sera are separated for assay by the cylinder plate method[4]. |
References: [1]. Tanaka N, et al. Mechanism of action of bicyclomycin. J Antibiot (Tokyo). 1976 Feb;29(2):155-68. | |
| Cas No. | 37134-40-0 | SDF | |
| 别名 | 双环霉素苯酸盐,FR2054 | ||
| 化学名 | 3'-benzoate bicyclomycin | ||
| Canonical SMILES | O=C1[C@@](O)(NC2=O)C(CCO[C@]2([C@@H](O)[C@@](C)(O)COC(C3=CC=CC=C3)=O)N1)=C | ||
| 分子式 | C19H22N2O8 | 分子量 | 406.4 |
| 溶解度 | DMSO : 100 mg/mL (246.07 mM; Need ultrasonic) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4606 mL | 12.3031 mL | 24.6063 mL |
| 5 mM | 0.4921 mL | 2.4606 mL | 4.9213 mL |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4606 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet