Tilbroquinol
(Synonyms: 甲溴羟喹) 目录号 : GC37792
Tilbroquinol具有抗原生动物活性，可作用于霍乱杆菌。
Cas No.:7175-09-9
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');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tilbroquinol is an antiprotozoal agent effective against amoebiasis. It has also been used against Vibrio cholerae.IC50 Value: Target: Antiparasitic
[1]. Bougoudogo, F, Fournier, J. M.; Dodin, A. "In vitro sensitivity of Vibrio cholerae serotype 0:139 to an intestinal antiseptic tiliquinol-tilbroquinol combination". Bulletin de la Societe de pathologie exotique (1990) 87 (1): 38-40. [2]. International Drug Names
| Cas No. | 7175-09-9 | SDF | |
| 别名 | 甲溴羟喹 | ||
| Canonical SMILES | OC1=C2N=CC=CC2=C(C)C=C1Br | ||
| 分子式 | C10H8BrNO | 分子量 | 238.08 |
| 溶解度 | DMSO: ≥ 50 mg/mL (210.01 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 4.2003 mL | 21.0013 mL | 42.0027 mL |
| 5 mM | 0.8401 mL | 4.2003 mL | 8.4005 mL |
| 10 mM | 0.42 mL | 2.1001 mL | 4.2003 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。
A screen for and validation of prodrug antimicrobials
Antimicrob Agents Chemother 2014;58(3):1410-9.PMID:24342644DOI:10.1128/AAC.02136-13.
The rise of resistant pathogens and chronic infections tolerant to antibiotics presents an unmet need for novel antimicrobial compounds. Identifying broad-spectrum leads is challenging due to the effective penetration barrier of Gram-negative bacteria, formed by an outer membrane restricting amphipathic compounds, and multidrug resistance (MDR) pumps. In chronic infections, pathogens are shielded from the immune system by biofilms or host cells, and dormant persisters tolerant to antibiotics are responsible for recalcitrance to chemotherapy with conventional antibiotics. We reasoned that the dual need for broad-spectrum and sterilizing compounds could be met by developing prodrugs that are activated by bacterium-specific enzymes and that these generally reactive compounds could kill persisters and accumulate over time due to irreversible binding to targets. We report the development of a screen for prodrugs, based on identifying compounds that nonspecifically inhibit reduction of the viability dye alamarBlue, and then eliminate generally toxic compounds by testing for cytotoxicity. A large pilot of 55,000 compounds against Escherichia coli produced 20 hits, 3 of which were further examined. One compound, ADC111, is an analog of a known nitrofuran prodrug nitrofurantoin, and its activity depends on the presence of activating enzymes nitroreductases. ADC112 is an analog of another known antimicrobial Tilbroquinol with unknown mechanism of action, and ADC113 does not belong to an approved class. All three compounds had a good spectrum and showed good to excellent activity against persister cells in biofilm and stationary cultures. These results suggest that screening for overlooked prodrugs may present a viable platform for antimicrobial discovery.
Elimination of a virulence plasmid from Shigella sonnei and Escherichia coli by antibiotics
Ann Inst Pasteur Microbiol 1986 Nov-Dec;137B(3):291-5.PMID:3318870DOI:10.1016/s0769-2609(86)80119-3.
Plasmid pWR105 is a non-self-conjugative plasmid conferring enteroinvasive properties on Shigella sonnei. Loss of this plasmid is accompanied by loss of the invasive phenotype as well as of the form I antigen expression. Thirteen antibiotics belonging to different chemical families were used at subinhibitory concentrations to eliminate pWR105 from S. sonnei and Escherichia coli K12. Rifampicin, novobiocin, chloramphenicol, cotrimoxazole and erythromycin eliminated the plasmid from both strains. Clindamycin eliminated pWR105 from E. coli only. Several other antibiotics gave a low rate of cure (ciprofloxacin, nalidixic acid, oxolinic acid, nifurzide, Tilbroquinol, minocycline). We may expect that these antibiotics would destabilize plasmids from other Shigella species and enteroinvasive E. coli, as these extrachromosomal DNA molecules share a high degree of homology.
[The role of 4-quinolones and antibiotics in the elimination of virulence plasmids of Enterobacteriaceae]
Pathol Biol (Paris) 1987 Dec;35(10 Pt 2):1386-8.PMID:3325901doi
Twenty-six antibiotics belonging to thirteen different chemical families had been tested on seven Enterobacteriaceae harbouring a virulence plasmid (Shigella sonnei, S. flexneri, S. dysenteriae, Escherichia coli (two plasmids). Yersinia and Salmonella dublin). Novobiocin and rifampicin were found to be most efficient eliminating three plasmids of which two come from Shigella. Clindamycin, cotrimoxazole, nifurzide, ciprofloxacin, and Tilbroquinol were also efficient, but at lower rate. Four virulence plasmids (from the three Shigella sp and Y. pestis) were eliminated by one or several antibiotics. The frequency of elimination was low (at best 10% bacteria per generation). The plasmid pWR105 from S. sonnei was the less stable.