Teclozan
(Synonyms: 替克洛占,WIN 13146) 目录号 : GC63904Teclozan (WIN 13146) 是一种抗原虫剂,属于苄胺衍生物类。Teclozan 干预磷脂代谢,阻止花生四烯酸的形成。Teclozan 在肠腔中起作用,可有效抗 G. intestinalis。Teclozan 可用于原生动物感染的研究。
Cas No.:5560-78-1
Sample solution is provided at 25 µL, 10mM.
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Teclozan (WIN 13146) is an antiprotozoal agent, class in benzylamine derivatives. Teclozan intervenes in the phospholipid metabolism preventes the formation of arachidonic acid. Teclozan acts in the intestinal lumen being effective in Anti-G. intestinalis. Teclozan can be used for the research of protozoan infections[1][2].
[1]. Gonzales MLM, et al. Antiamoebic drugs for treating amoebic colitis. Cochrane Database Syst Rev. 2019;1(1):CD006085. Published 2019 Jan 9.
[2]. DÍaz, V. M. M. . Pharmacological Treatment of Giardiasis. In: Rodriguez-Morales, A. J. , editor. Current Topics in Giardiasis [Internet]. London: IntechOpen; 2017.
Cas No. | 5560-78-1 | SDF | Download SDF |
别名 | 替克洛占,WIN 13146 | ||
分子式 | C20H28Cl4N2O4 | 分子量 | 502.26 |
溶解度 | DMSO : 62.5 mg/mL (124.44 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.991 mL | 9.955 mL | 19.91 mL |
5 mM | 0.3982 mL | 1.991 mL | 3.982 mL |
10 mM | 0.1991 mL | 0.9955 mL | 1.991 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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Activity of quinfamide against natural infections of Entamoeba criceti in hamsters: a new potent agent for intestinal amoebiasis
Parasitology 1980 Aug;81(1):157-68.PMID:6252530DOI:10.1017/s0031182000055128.
A novel tetrahydroquinolinyl ester, quinfamide, administered orally in multiple doses for 3 days had an ED50 of 0.25 mg/kg/day (total dose 0.75 mg/kg) for eradicating Entamoeba criceti in hamsters in several tests. It was significantly more active by direct comparison than 3 commercially available amoebicides and at least as active as 2 other esters of the parent compound, 1-(dichloroacety)-1,2,3,4-tetrahydro-6-quinolinol. After administration of a single dose, ED50 calculations for quinfamide averaged 0.9 mg/kg. Quinfamide was considerably more active than the other tetrahydroquinolinols, diloxanide furoate and Teclozan, and it was approximately 1.5 times more active than etofamide; a statistical significance between the latter 2 drugs could be demonstrated in one of 4 tests. Administered prophylactically, quinfamide was shown to protect hamsters from re-infection with E. criceti. It also inhibited propagation of E. histolytica in vitro at a concentration of 20 microgram/ml. No adverse effects were noted in rodents after a single dose as high as 10 g/kg. Daily administration to monkeys of doses up to 500 mg/kg for as long as 37 days produced no pharmacological aberrations during or after medication; haematological studies and urine analyses were normal and no gross or microscopical tissue changes attributable to quinfamide were observed. No toxicity was revealed following acute (2 g/kg) and chronic (500 mg/kg/day x 31 days) administration of the drug to dogs and rats, respectively.
[Evaluation of the tolerance and efficiency of quinfamide, a new intraluminal amebicide, in man (one day treatment). Double blind study]
Rev Gastroenterol Mex 1980 Apr-Jun;45(2):93-7.PMID:7403767doi
A new intraluminal amebicide (Quinfamide) was tested to assess its effectivity and tolerance for treatment of non-dysenteric intestinal amebiasis. The drug was administered to three groups of ten patients each, whom received 300, 600 and 1 200 mg. on a 24 hours schedule. Another group of ten patients received Teclozan as control drug. Diagnosis and results were judged by rectosigmoidoscopy before, 15 and 30 days after treatment. In addition, microscopic investigation of ameba was performed in freshly passed stools, before, and after 8, 15 and 30 days of treatment. Success after treatment with the three doses of Quinfamide was obtained in 89.2% of the cases. Side reactions were clinically non-significant. More experience is needed before the effectivity of the drug is stablished.