Mefloquine hydrochloride (Mefloquin hydrochloride) 是一种喹啉抗疟药,是一种抗SARS-CoV-2进入抑制剂。Mefloquine hydrochloride 也是一种 K+通道 (KvQT1/minK) 拮抗剂,IC50为 ~1 μM。Mefloquine hydrochloride 可用于疟疾、系统性红斑狼疮和癌症的研究。
生物活性 | Mefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2entry inhibitor. Mefloquine hydrochloride is also aK+channel (KvQT1/minK)antagonist with anIC50of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus andcancerresearch[1][2][3]. |
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体外研究 (In Vitro) | Mefloquine hydrochloride selectively inhibits prostate cancer (PCa) cell growth with an IC50of ~10 μM. Mefloquine hydrochloride also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation[2]. Mefloquine hydrochloride (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells[2]. Mefloquine shows higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50of 1.28 μM, IC90of 2.31 μM, and IC99of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell[3].
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体内研究 (In Vivo) | Mefloquine hydrochloride (5 mg/kg; i.p.; daily; 14 days) reverses the lower vertebral cancellous bone volume and bone formation; and has modest effects on cortical bone volume, thickness, and moment of inertia in old mice[4].
Animal Model: | Young 3.5-month-old and old 21-month-old female C57BL/6 mice[4] | Dosage: | 5 mg/kg | Administration: | Intraperitoneal injection; daily; 14 days | Result: | Reversed the lower vertebral cancellous bone volume and bone formation in old mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(120.55 mM;Need ultrasonic) H2O : 2.86 mg/mL(6.90 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.4110 mL | 12.0549 mL | 24.1097 mL | 5 mM | 0.4822 mL | 2.4110 mL | 4.8219 mL | 10 mM | 0.2411 mL | 1.2055 mL | 2.4110 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.03 mM) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.03 mM) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.03 mM) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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