Ferroquine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ferroquine (Ferrochloroquine)，是 Chloroquine 的二茂铁基类似物，是一种抗疟疾剂。Ferroquine 通过诱导氧化应激和随后的膜破坏而对疟原虫表现出杀虫作用。

Ferroquine (Ferrochloroquine), a ferrocenyl analogue of Chloroquine, is an antimalarial agent. Ferroquine shows parasiticidal effect on Plasmodium by inducing oxidative stress and the subsequent destruction of the membrane.

Ferroquine shows cytotoxicity against non-cancerous MRC-5 and HeLa cancer cells with IC50 values of 24.4 μM and 16.8 μM, respectively.24?hours post-incubation all newly transformed schistosomula (NTS)exposed to 33.3?μM Ferroquine shows strongly reduced viabilities.

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 ofChloroquine (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.

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Other Targets

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185055-67-8

433.76

C23H24ClFeN3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 4.35 mg/mL (10.03 mM; 超声助溶 (<60°C)

ClC1=CC2=NC=CC(NC[C-]34[CH]5=[CH]6[CH]7=C3([Fe+2]675489%10%11[CH]%12=[CH]8[CH-]9[CH]%10=[CH]%12%11)CN(C)C)=C2C=C1

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(-20℃)

With Ice Pack

≥ 2 years