Ferroquine (Ferrochloroquine)
(Synonyms: 二茂铁氯喹; Ferrochloroquine; SSR97193) 目录号 : GC32125
Ferroquine (Ferrochloroquine) (Ferrochloroquine) 是 Chloroquine 的二茂铁类似物，是一种抗疟药。
Cas No.:185055-67-8
Sample solution is provided at 25 µL, 10mM.
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Ferroquine is an ingenious antimalarial agent.
The 24 hours post-incubation all newly transformed schistosomula (NTS) exposed to 33.3 µM Ferroquine (FQ), hydroxyl-ferroquine (FQ-OH) and Ruthenoquine (RQ) shows strongly reduced viabilities. 72 hours post-incubation all NTS exposed to 33.3 µM RQ have died, while Ferroquine and FQ-OH treated worms are strongly affected but still alive[1].
Treatment of mice with 200 and 800 mg/kg Ferroquine, shows low total worm burden reductions of 19.4% and 35.6%. One of the mice treated with 800 mg/kg Ferroquine died within 24 hours post-treatment. No activity is observed treating mice with RQ at 200 mg/kg. Finally, a total worm burden reduction of 17.3% is observed following treatment with FQ-OH. Hence, modification of Chloroquine (CQ) by a ferrocenyl or ruthenocenyl fragment does not increase the antischistosomal properties of CQ. For comparison, at 200 mg/kg mefloquine (MQ) achieves a much higher worm burden reduction of 72.3% in S. mansoni-infected mice. A higher effect against female adult S. mansoni is also observed in MQ treated mice pointing to a sex-specific interference of these drugs with the target. Furthermore, in one of the FQ-OH treated mice many dead worms are recovered and a hepatic shift (i.e. worms migrating to the liver) observed. Hence, Ferroquine and FQ-OH show weak antischistosomal activity in vivo[1].
[1]. Keiser J, et al. In vitro and in vivo antischistosomal activity of ferroquine derivatives. Parasit Vectors. 2014 Sep 4;7:424.
Cell experiment: | Cytotoxicity studies are performed on human cervix HeLa cancer cells and non tumorigenic human fetal lung fibroblasts MRC-5 to compare the activity of Ferroquine, RQ, FQ-OH, CQ, MQ and Cisplatin. The cell viability is determined via a colorimetric cell-based assay using Resazurin. Briefly, one day before treatment cells are plated in triplicates in 96-well plates at a density of 4 × 103 cells/well in 100 µL. Upon treating cells with increasing concentrations of the target complexes (freshly prepared stock solution in DMSO), cells are incubated at 37°C/6% CO2 for 48 h, the medium is removed, and 100 µL of complete medium containing resazurin (0.2 mg/mL final concentration) is added. After 4 h of incubation at 37°C/6% CO2, the fluorescence of the highly red fluorescent resorufin product is quantified at 590 nm emission with 540 nm excitation wavelength in a SpectraMax M5 microplate Reader[1]. |
Animal experiment: | Mice[1] Groups of 3-4 NMRI mice are treated orally with single oral doses of 200 mg/kg of Ferroquine, FQ-OH and RQ. In addition, one group of mice is treated with a single oral dose of 800 mg/kg Ferroquine. Untreated mice serve as controls in all experiments. At 21 d post-treatment, animals are killed by the CO2 method and dissected. Worms are removed by picking, then sexed and counted. |
References: [1]. Keiser J, et al. In vitro and in vivo antischistosomal activity of ferroquine derivatives. Parasit Vectors. 2014 Sep 4;7:424. | |
| Cas No. | 185055-67-8 | SDF | |
| 别名 | 二茂铁氯喹; Ferrochloroquine; SSR97193 | ||
| Canonical SMILES | ClC1=CC=C2C(NC[C-]34[Fe+2]56789%10%11([CH-]%12[CH]8=[CH]9[CH]%10=[CH]%11%12)C3(CN(C)C)=[CH]5[CH]6=[CH]47)=CC=NC2=C1 | ||
| 分子式 | C23H24ClFeN3 | 分子量 | 433.75 |
| 溶解度 | DMSO : 8.33 mg/mL (19.20 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3055 mL | 11.5274 mL | 23.0548 mL |
| 5 mM | 0.4611 mL | 2.3055 mL | 4.611 mL |
| 10 mM | 0.2305 mL | 1.1527 mL | 2.3055 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