产品说明书

Clioquinol

Print
Chemical Structure| 130-26-7 同义名 : 5-氯-7-碘-8-羟基喹啉 ;Iodochlorohydroxyquinoline;Iodochlorohydroxyquin;NSC 74938;NSC 3531;Chinoform;Iodochlorhydroxyquin
CAS号 : 130-26-7
货号 : A147542
分子式 : C9H5ClINO
纯度 : 98% T
分子量 : 305.5
MDL号 : MFCD00006787
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(163.67 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 18 mg/mL suspension

生物活性
描述 Clioquinol is an antiseptic drug and is effective against multidrug-resistant Candida. Clioquinol prevented more than 90 % of biofilm formation, which can be attributed to blockade of hyphal development. Clioquinol also reduced the metabolic activity of sessile Candida but the susceptibility was lower compared to planktonic cells (0.031 - 0.5 µg/ml required to inhibit 50 % planktonic cells and 4 - 16 µg/ml to inhibit 50% preformed biofilms)[3]. Clioquinol fully protected D. melanogaster from the infection. Effective concentration found in modelling indicated that clioquinol was highly effective against C. albicans (0.306 μg/mL) in easily achievable serum levels; clioquinol rapidly achieved kill rate reaching the maximum effect after 13 hours[4]. The antimicrobial strength of 3% clioquinol cream depended on the species but it can act on most of the species. It could inhibit the growth of most fungal species with different strength, but the antibacterial activity was weak. For Candida tropicalis, Candida guilliermondii, Aspergillus terreus, Fusarium solani and Trichoderma harzianum, the inhibition zone was biggest among all the tested drugs. The antifungal activity for Dermatophytes and Candida albicans was moderate[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00943748 Parkinson's Disease Phase 2 Phase 3 Completed - France ... 展开 >> Service de Neurologie, Clinique Neurologique, EA 2683, IFR 114 Lille, France, 59037 收起 <<
NCT01429701 Eczema Phase 3 Completed - -
NCT00963495 Acute Myeloid Leukemia ... 展开 >> Acute Lymphocytic Leukemia Chronic Lymphocytic Leukemia Myelodysplasia Lymphoma, Non-Hodgkin Hodgkin's Lymphoma Multiple Myeloma 收起 << Phase 1 Terminated - Canada, Ontario ... 展开 >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.27mL

0.65mL

0.33mL

16.37mL

3.27mL

1.64mL

32.73mL

6.55mL

3.27mL
参考文献

[1]Yu H, Zhou Y, et al. Clioquinol targets zinc to lysosomes in human cancer cells. Biochem J. 2009 Jan 1;417(1):133-9.

[2]Pollera C, Lucchini B, et al. Evaluation of anti-prionic activity of clioquinol in an in vivo model (Mesocricetus auratus). Vet Res Commun. 2005 Aug;29 Suppl 2:253-5.

[3]Pippi B, Machado GDRM, Bergamo VZ, Alves RJ, Andrade SF, Fuentefria AM. Clioquinol is a promising preventive morphological switching compound in the treatment of Candida infections linked to the use of intrauterine devices. J Med Microbiol. 2018;67(11):1655‐1663

[4]Pippi B, Merkel S, Staudt KJ, et al. Oral clioquinol is effective in the treatment of a fly model of Candida systemic infection. Mycoses. 2019;62(5):475‐481

[5]You Z, Ran X, Dai Y, Ran Y. Clioquinol, an alternative antimicrobial agent against common pathogenic microbe. J Mycol Med. 2018;28(3):492‐501