Ferroquine (Ferrochloroquine) |
| Katalog-Nr.GC32125 |
Ferroquin (Ferrochloroquin) (Ferrochloroquin), ein Ferrocenyl-Analogon von Chloroquin, ist ein Malariamittel.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| 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 | ||
| Formula | C23H24ClFeN3 | M.Wt | 433.75 |
| Löslichkeit | DMSO : 8.33 mg/mL (19.20 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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