Diiodohydroxyquinoline (Iodoquinol)
(Synonyms: 5,7-二碘-8-羟基喹啉,Iodoquinol; 5,7-Diiodo-8-hydroxyquinoline; 5,7-Diiodo-8-quinolinol) 目录号 : GC32171Diiodohydroxyquinoline (Iodoquinol) is a topical therapeutic agent,a quinoline derivative, with satisfactory antibacterial properties.
Cas No.:83-73-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Datasheet
Diiodohydroxyquinoline (Iodoquinol) is a topical therapeutic agent,a quinoline derivative, with satisfactory antibacterial properties.
Cas No. | 83-73-8 | SDF | |
别名 | 5,7-二碘-8-羟基喹啉,Iodoquinol; 5,7-Diiodo-8-hydroxyquinoline; 5,7-Diiodo-8-quinolinol | ||
Canonical SMILES | OC1=C2N=CC=CC2=C(I)C=C1I | ||
分子式 | C9H5I2NO | 分子量 | 396.95 |
溶解度 | DMSO : 25 mg/mL (62.98 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。 |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5192 mL | 12.596 mL | 25.1921 mL |
5 mM | 0.5038 mL | 2.5192 mL | 5.0384 mL |
10 mM | 0.2519 mL | 1.2596 mL | 2.5192 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。
Balantioides coli
Res Vet Sci 2021 Mar;135:424-431.PMID:33183780DOI:10.1016/j.rvsc.2020.10.028.
Balantioides coli (=Balantidium coli) is the only ciliate that parasitizes humans. Pigs are the main reservoir. Other species, as camels, cattle, donkey, sheep and goat have been also proposed as reservoirs for human infections. The parasite has a direct life cycle, being transmitted by the faecal-oral route. This type of cycle and the large number of host species imply an important potential for zoonotic transmission of the parasite. Infections are most commonly found in tropical and temperate regions, with prevalence up to 100% in pigs; high prevalence values have been also recorded in some non-human primates and camels. In humans, prevalence is usually under 10% in the population at risk. The main epidemiological factors involved in the transmission of this parasite include close contact with pigs, lack of basic sanitation infrastructures (water supply, wastewater disposal) and hygiene. Individual health status, intestinal microbiota and diet are also important for the onset of the infection. Outbreaks caused by this parasite are rare; those reported to date were related to poor hygienic conditions or to catastrophic natural disasters. Balantioides coli infections can be asymptomatic and symptomatic, which can be chronic (with intermittent diarrhoea), or acute (a dysenteric form which can be life-threatening). Efective treatments include tetracycline, Iodoquinol and 5-nitroimidazole compounds (metronidazole, secnidazole). The main effective individual preventive measure is the use of disinfected water for drinking and other uses. Adequate water supply infrastructures, proper disposal of wastewater and animal faeces, and regular monitoring programs on farms will help limit transmission.
Amoebic dysentery
BMJ Clin Evid 2013 Aug 30;2013:0918.PMID:23991750doi
Introduction: Amoebic dysentery is caused by the protozoan parasite Entamoeba histolytica. It is transmitted in areas where poor sanitation allows contamination of drinking water and food with faeces. In these areas, up to 40% of people with diarrhoea may have amoebic dysentery. Methods and outcomes: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of drug treatments for amoebic dysentery in endemic areas? We searched: Medline, Embase, The Cochrane Library, and other important databases up to June 2013 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA). Results: We found 6 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions. Conclusions: In this systematic review, we present information relating to the effectiveness and safety of the following interventions: Diiodohydroxyquinoline (Iodoquinol), diloxanide, emetine, metronidazole, nitazoxanide, ornidazole, paromomycin, secnidazole, and tinidazole.
Amoebic dysentery
BMJ Clin Evid 2011 Jan 13;2011:0918.PMID:21477391doi
Introduction: Amoebic dysentery is caused by the protozoan parasite Entamoeba histolytica. It is transmitted in areas where poor sanitation allows contamination of drinking water and food with faeces. In these areas, up to 40% of people with diarrhoea may have amoebic dysentery. Methods and outcomes: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of drug treatments for amoebic dysentery in endemic areas? We searched: Medline, Embase, The Cochrane Library, and other important databases up to April 2010 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA). Results: We found 6 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions. Conclusions: In this systematic review, we present information relating to the effectiveness and safety of the following interventions: Diiodohydroxyquinoline (Iodoquinol), diloxanide, emetine, metronidazole, nitazoxanide, ornidazole, paromomycin, secnidazole, and tinidazole.
Identification and Characterization of the Human Cytosolic Sulfotransferases Mediating the Sulfation of Clioquinol and Iodoquinol
Drug Metab Lett 2016;10(3):200-205.PMID:27449410DOI:10.2174/1872312810666160719142850.
Objective: The aim of the current study was to identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating clioquinol and Iodoquinol, and to verify the presence of clioquinol/ iodoquinol-sulfating activity in human organ homogenates and cultured cells. Method: An established sulfotransferase assay was employed to analyze clioquinol/iodoquinolsulfating activity of thirteen known human SULTs, as well as cytosols of human kidney, liver, lung, and small intestine. Metabolic labeling with [35S]sulfate in the presence of different concentrations of clioquinol/Iodoquinol was performed using cultured HepG2 human hepatoma cells and Caco-2 human colon carcinoma cells. Results: A systematic analysis revealed that six of the thirteen known human SULTs, SULT1A1 SULT1A2, SULTA3, SULT1B1, SULT1C4, and SULT1E1 showed considerable clioquinol/ iodoquinol-sulfating activity. Kinetic parameters of the sulfation of clioquinol and Iodoquinol by three SULTs, SULT1A1, SULT1A3, and SULT1C4, that showed the strongest clioquinol/iodoquinolsulfating activity were determined. Moreover, clioquinol/iodoquinol-sulfating activity was detected in the cytosol fractions of human liver, lung, kidney, and small intestine. Cultured HepG2 and Caco-2 cells were shown to be capable of sulfating clioquinol/Iodoquinol under metabolic conditions. Conclusion: Collectively, these results provided a molecular basis underling the metabolism of clioquinol and Iodoquinol through sulfation.
Repurposing the Antiamoebic Drug Diiodohydroxyquinoline for Treatment of Clostridioides difficile Infections
Antimicrob Agents Chemother 2020 May 21;64(6):e02115-19.PMID:32253206DOI:10.1128/AAC.02115-19.
Clostridioides difficile, the leading cause of nosocomial infections, is an urgent health threat worldwide. The increased incidence and severity of disease, the high recurrence rates, and the dearth of effective anticlostridial drugs have created an urgent need for new therapeutic agents. In an effort to discover new drugs for the treatment of Clostridioides difficile infections (CDIs), we investigated a panel of FDA-approved antiparasitic drugs against C. difficile and identified Diiodohydroxyquinoline (DIHQ), an FDA-approved oral antiamoebic drug. DIHQ exhibited potent activity against 39 C. difficile isolates, inhibiting growth of 50% and 90% of these isolates at concentrations of 0.5 渭g/ml and 2 渭g/ml, respectively. In a time-kill assay, DIHQ was superior to vancomycin and metronidazole, reducing a high bacterial inoculum by 3 log10 within 6 h. Furthermore, DIHQ reacted synergistically with vancomycin and metronidazole against C. difficilein vitro. Moreover, at subinhibitory concentrations, DIHQ was superior to vancomycin and metronidazole in inhibiting two key virulence factors of C. difficile, toxin production and spore formation. Additionally, DIHQ did not inhibit the growth of key species that compose the host intestinal microbiota, such as Bacteroides, Bifidobacterium, and Lactobacillus spp. Collectively, our results indicate that DIHQ is a promising anticlostridial drug that warrants further investigation as a new therapeutic for CDIs.