Ferroquine-Ferrochloroquine-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFerroquineCat. No.: HY-19364CAS No.: 185055-67-8Synonyms: Ferrochloroquine; SSR97193分式: CHClFeN分量: 433.75作靶点: Parasite作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 8.33

2、 mg/mL (19.20 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3055 mL 11.5274 mL 23.0548 mL5 mM 0.4611 mL 2.3055 mL 4.6110 mL10 mM 0.2305 mL 1.1527 mL 2.3055 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议

3、您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (1.91 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (1.91 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Mast

4、er of Small Molecules 您边的抑制剂师www.MedChemESolubility: 0.83 mg/mL (1.91 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ferroquine种巧妙的抗疟药。IC50 & Target antimalarial 1体外研究 The 24hours post-incubation all newly transformed schistosomula (NTS) exposed to 33.3M Ferroquine(FQ), hydroxyl-ferroquine (FQ-OH) and Ru

5、thenoquine (RQ) shows strongly reduced viabilities. 72hours post-incubation all NTS exposed to 33.3 M RQ have died, while Ferroquine and FQ-OH treated worms arestrongly affected but still alive 1.体内研究 Treatment of mice with 200 and 800mg/kg Ferroquine, shows low total worm burden reductions of 19.4%

6、and 35.6%. One of the mice treated with 800mg/kg Ferroquine died within 24hours post-treatment. Noactivity is observed treating mice with RQ at 200mg/kg. Finally, a total worm burden reduction of 17.3% isobserved following treatment with FQ-OH. Hence, modification of Chloroquine (CQ) by a ferrocenyl

7、 orruthenocenyl fragment does not increase the antischistosomal properties of CQ. For comparison, at 200mg/kg mefloquine (MQ) achieves a much higher worm burden reduction of 72.3% in S. mansoni-infectedmice. A higher effect against female adult S. mansoni is also observed in MQ treated mice pointing

8、 to a sex-specific interference of these drugs with the target. Furthermore, in one of the FQ-OH treated mice manydead worms are recovered and a hepatic shift (i.e. worms migrating to the liver) observed. Hence, Ferroquineand FQ-OH show weak antischistosomal activity in vivo 1.PROTOCOLCell Assay 1 C

9、ytotoxicity studies are performed on human cervix HeLa cancer cells and non tumorigenic human fetal lungfibroblasts MRC-5 to compare the activity of Ferroquine, RQ, FQ-OH, CQ, MQ and Cisplatin. The cell viabilityis determined via a colorimetric cell-based assay using Resazurin. Briefly, one day befo

10、re treatment cells areplated in triplicates in 96-well plates at a density of 4103 cells/well in 100L. Upon treating cells withincreasing concentrations of the target complexes (freshly prepared stock solution in DMSO), cells areincubated at 37C/6% CO2 for 48h, the medium is removed, and 100L of com

11、plete medium containingresazurin (0.2mg/mL final concentration) is added. After 4h of incubation at 37C/6% CO2, the fluorescenceof the highly red fluorescent resorufin product is quantified at 590nm emission with 540nm excitationwavelength in a SpectraMax M5 microplate Reader 1.MCE has not independe

12、ntly confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Groups of 3-4 NMRI mice are treated orally with single oral doses of 200mg/kg of Ferroquine, FQ-OH andRQ. In addition, one group of mice is treated with a single oral dose of 800mg/kg Ferroquine.

13、Untreated miceserve as controls in all experiments. At 21 d post-treatment, animals are killed by the CO2 method anddissected. Worms are removed by picking, then sexed and counted.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Keiser J, et al. In vitro and in vivo antischistosomal activity of ferroquine derivatives. Parasit Vectors. 2014 Sep 4;7:424