Melarsonyl (Melarsonic acid)
(Synonyms: Melarsonic acid) 目录号 : GC32357Melarsonyl (Melarsonic acid) (Melarsonic acid) 是一种驱虫剂,能有效抑制寄生虫。
Cas No.:37526-80-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[1]Mice are infected i.p. with 104 bloodstream trypomastigotes taken from an infected mouse and suspended in 0.1 mL of phosphate-buffered saline, pH 7.2. The infection is allowed to develop for 24 h before treatment is begun. Ten infected mice are used as controls and received only excipient, 1% carboxymethylcellulose by the i.p. route in a 0.1 ml volume. The other mice receive a single dose of the diluted or suspended Potassium Melarsonyl (20, 40, 60 μmol/kg) in the same manner. Six mice are used per dose. The trypanocidal activity is evaluated by the mean survival time of treated mice for each dose[1]. |
References: [1]. Loiseau PM, et al. Contribution of dithiol ligands to in vitro and in vivo trypanocidal activities of dithiaarsanes and investigation of ligand exchange in an aqueous solution. Antimicrob Agents Chemother. 2000 Nov;44(11):2954-61. |
Melarsonyl (Melarsonic acid) is an anthelmintic agent which can inhibit parasite potently.
For acute infections produced by T. brucei brucei GVR, Potassium Melarsonyl exhibits trypanocidal activities. Potassium Melarsonyl (Trimelarsan) cures less than 50% mice at a dose of 25 μmol/kg for 4 consecutive days. At 60 μmol/kg, it cures all the mice in a chronic-infection model[1].
[1]. Loiseau PM, et al. Contribution of dithiol ligands to in vitro and in vivo trypanocidal activities of dithiaarsanes and investigation of ligand exchange in an aqueous solution. Antimicrob Agents Chemother. 2000 Nov;44(11):2954-61.
Cas No. | 37526-80-0 | SDF | |
别名 | Melarsonic acid | ||
Canonical SMILES | O=C(C1S[As](C2=CC=C(NC3=NC(N)=NC(N)=N3)C=C2)SC1C(O)=O)O | ||
分子式 | C13H13AsN6O4S2 | 分子量 | 456.33 |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1914 mL | 10.957 mL | 21.914 mL |
5 mM | 0.4383 mL | 2.1914 mL | 4.3828 mL |
10 mM | 0.2191 mL | 1.0957 mL | 2.1914 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。
Evaluation of DL-alpha-difluoromethylornithine against susceptible and drug-resistant Trypanosoma brucei brucei
Acta Trop 1991 Jan;48(3):223-32.PMID:1671624DOI:10.1016/0001-706x(91)90050-t.
The antitrypanosomal activity of the ornithine decarboxylase inhibitor DL-alpha-difluoromethylornithine (DFMO, eflornithine) was tested in ten stocks and one clone of the hemoflagellate Trypanosoma brucei brucei in an in vitro system. They showed varying levels of susceptibility to DFMO, their IC50 (the concentration which inhibited growth by 50%) values ranging from 81-691 microM. Differences in DFMO susceptibility were also demonstrated in mice. Combinations of Melarsonyl potassium (mel W; trimelarsan) and DFMO showed an additive effect in vitro in a mel W-susceptible and a mel W-resistant stock, but an antagonistic effect in a mel W- and DFMO-susceptible clone. Combinations of suramin and DFMO showed an antagonistic effect in vitro in a suramin-susceptible clone, but a potentiation in a suramin-resistant stock.