产品说明书
Mefloquine HCI
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同义名 : | Mefloquin hydrochloride;Mefloquine (hydrochloride);Ro 21-5998/001;NSC 157387;Mefloquine HCl |
| CAS号 : | 51773-92-3 | |
| 货号 : | A192274 | |
| 分子式 : | C17H17ClF6N2O | |
| 纯度 : | 99% | |
| 分子量 : | 414.773 | |
| MDL号 : | MFCD00797519 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(120.55 mM)，配合低频超声助溶，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 H2O: 2.5 mg/mL(6.03 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Mefloquine (Hydrochloride) is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. Mefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. Mefloquine can prolong cardiac repolarization, especially when coadministered with halofantrine, an antagonist of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Using patch-clamp electrophysiology we found that mefloquine inhibited KvLQT1/minK channel currents with an IC50 value of approximately 1 microM[2]. Mefloquine possesses activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria[3]. The anti-malarial mefloquine was previously shown to be active against E. multilocularis metacestodes in vitro, and in mice infected by intraperitoneal inoculation of metacestodes when administered at 100 mg/kg by oral gavage twice a week for 12 weeks. After 12 weeks of treatment, the presence of parasite lesions was assessed in a liver squeeze chamber and by PCR, and a significantly reduced parasite load was found in mefloquine-treated animals[4]. Mefloquine (MQ) has a highly selective cytotoxicity that inhibits PCa (prostate cancer) cell growth. MQ also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS (reactive oxygen species) generation[1]. | ||
| 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 |
| NCT01976325 | Malaria | Not Applicable | Unknown | November 2015 | Canada, Ontario ... 展开 >> National Capital Region Occupational Health Clinic Recruiting Ottawa, Ontario, Canada, K1A 0K9 Contact: Louise J Levesque, RN, BScN 613-946-5533 louise.j.levesque@hc-sc.gc.ca Contact: Lisa Taras, MD, CCFP 613-946-6583 lisa.taras@hc-sc.gc.ca Ottawa Hospital Research Institute Recruiting Ottawa, Ontario, Canada, K1Y 4E9 Contact: Charde A Morgan, MScPH 613-737-8899 ext 72424 cmorgan@ohri.ca Contact: Anne E McCarthy, MD 613-737-8899 ext 78184 amccarthy@toh.on.ca Principal Investigator: Anne E McCarthy, MD, MSc Sub-Investigator: Charde A Morgan, MScPH International Association for Medical Assistance to Travellers Recruiting Toronto, Ontario, Canada, M6K 3E3 Contact: Tullia Marcolongo 416-652-0137 tullia@iamat.org 收起 << |
| NCT00902811 | Uncomplicated Falciparum Malar... 展开 >>ia 收起 << | Phase 4 | Unknown | December 2009 | Myanmar ... 展开 >> Dabhine and Mingan Clinic Recruiting Sittwe, Rakhine, Myanmar Contact: Pyay Phyo Aung frank_smithuis@yahoo.com Principal Investigator: Pyay Phyo Aung, MD Myit Kyi Nar Clinic Recruiting Kachin, Myanmar Contact: Mya Nee Nyo frank_smithuis@yahoo.com Principal Investigator: Mya Nee Nyo, MD Myothugyi Rural Health Center, Bu Thee Daung Recruiting Maungdaw, Myanmar Contact: Arkar Linn Naing frank_smithuis@yahoo.com Principal Investigator: Arkar Linn Naing, MD Lashio Clinic Recruiting Shan, Myanmar Contact: Naing Nyo, MD Principal Investigator: Naing Zaw, MD 收起 << |
| NCT01107145 | Plasmodium Vivax Malaria | Phase 4 | Terminated(Extremely slow enro... 展开 >>llment) 收起 << | - | Brazil ... 展开 >> Hospital Geral Maternidade de Cruzeiro do Sul Cruzeiro do Sul, Acre, Brazil Hospital Municipal Teonila Alves Anajas, Para, Brazil Centro de Pesquisa em Patologias Tropicais Porto Velho, Rondonia, Brazil 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.05mL 2.41mL 1.21mL |
24.11mL 4.82mL 2.41mL |
| 参考文献 |
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