Lonidamine (AF-1890) 是一种己糖激酶 (hexokinase) 和丙酮酸载体 (mitochondrial pyruvate carrier) 抑制剂 (Ki: 2.5 μM)。Lonidamine 还可抑制癌细胞中的有氧糖酵解。Lonidamine 可用于线粒体代谢和炎症的研究，如肺纤维化。
| 生物活性 | Lonidamine (AF-1890) is ahexokinaseandmitochondrial pyruvate carrierinhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis incancercells. Lonidamine can be used in the research ofmitochondrial metabolismand inflammation, such as pulmonary fibrosis[1][2][3]. |
| IC50& Target | Ki: 2.5 μM (Mitochondrial pyruvate carrier)[2] |
体外研究
(In Vitro) | Lonidamine (100 μM, 24 h) inhibits TGF-β-stimulated lactate production and oxygen consumption rate in AKR-2B and TIG-1 cells[3].
Lonidamine (100 μM, 24/48 h) inhibits H2030BrM3 and A549 cell proliferation[4].
Lonidamine (100-200 μM, 24 h) inhibits H2030BrM3 and A549 cell invasion[4].
Lonidamine (100-1000 μM, 24 h) inhibits mitochondrial complex I and II activities[4].
Lonidamine (200 μM, 24 h) increases ROS generation in H2030BrM3 lung cancer cells[4].
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体内研究
(In Vivo) | Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model[3].
| Animal Model: | Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model[3].
| | Dosage: | 10, 30, 100 mg/kg/day | | Administration: | Oral administration, daily, d10 to d20 after BLM treatment. | | Result: | Partially or completely reversed the increases in HK2 and lactate induced by BLM and reduced the expression of 10 profibrotic mediators. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(155.69 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.1137 mL | 15.5686 mL | 31.1371 mL | | 5 mM | 0.6227 mL | 3.1137 mL | 6.2274 mL | | 10 mM | 0.3114 mL | 1.5569 mL | 3.1137 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。-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: ≥ 2.08 mg/mL (6.48 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.48 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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%corn oil Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.48 mM，饱和度未知) 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 20.8 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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