Lonidamine (AF-1890) 是一种口服的小分子己糖激酶（HK）抑制剂，也是一种CFTR开放通道阻断剂，IC50为0.85 mM。此外，Lonidamine也可改善阿尔茨海默病（AD）小鼠认知功能障碍。
别名：AF 1890；Diclondazolic Acid; DICA
Lonidamine (AF-1890) 是一种口服的小分子己糖激酶 (IC50=0.85 mM) 和丙酮酸载体 (mitochondrial pyruvate carrier) 抑制剂 (Ki=2.5 μM)。Lonidamine (Diclondazolic Acid) 同时也抑制线粒体复合物 II。Lonidamine 可用于线粒体代谢和炎症的研究，Lonidamine 还可抑制癌细胞中的有氧糖酵解。
. figure 14.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 14.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 assay | |
| 细胞系/动物模型 | HL60, MOLM13, NB4, and PBMC cells | |
| 浓度 | 1~100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | An overall higher degree of reduced metabolic activity was observed from three independent studies with MOLM13 (Figure 14A) and NB4 (Figure14B) cells thus were suggested being more responsive to co-treatment. HL60 cells responded revealed low response to both drugs alone,resulting in only 10-25 % reduced proliferation when exposed to the highest concentrations of VPA (1 mM) and LND (100 µM), respectively (Figure 14C). |
. figure 13.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 13.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | Cell viability assay | |
| 细胞系/动物模型 | HL60, MOLM13, NB4, and PBMC cells | |
| 浓度 | 1~100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | These data indicated a comparable trend of viability in all three cell lines following combinatorial treatment of VPA and LND (Figure 13B, C). HL60 cells are only presented for Hoechst viability scoring in figure 13A since the cells do not expose phosphatidylserine upon apoptosis induction. |
. figure 12.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 12.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | MST-1 proliferation assay | |
| 细胞系/动物模型 | HL60 cells | |
| 浓度 | 50 and 100 µM | |
| 处理时间 | 48 or 72 h | |
| 实验结果 | Maximal potentiation of LND was obtained by 100 µM LND in the sequence VPA LND+VPA, but no significant increased anti-proliferative effect was obtained from three independent and replicable studies. |
. figure 11.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 11.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | Hoechst 33342 staining | |
| 细胞系/动物模型 | HL60, MOLM13 and NB5 cells | |
| 浓度 | 0~500 µM | |
| 处理时间 | 24 or 48 h | |
| 实验结果 | LND elicits potential of inducing apoptosis after both 24 hours and 48 hour incubation at higher concentrations (> 50 µM) in HL60, MOLM13 and NB4 (Figure 11A-B). Apoptotic cells in the stage of morphological changes such as fragmented or condensed nuclei are shown in Figure 11C, visualized by fluorescence microscopy. |
. figure 10.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 10.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation assay | |
| 细胞系/动物模型 | HL60, MOLM13, NB4, and PBMC cells | |
| 浓度 | 0~1000 µM | |
| 处理时间 | 48 h | |
| 实验结果 | The distinct response of PBMC comparable to MOLM13 and HL60 is noticeably demonstrated in Figure 10A. NB4 was significantly (P<0.05) more sensitive to LND under 24 hours of exposure than 48 hours (5 – 500 µM). The IC50 of LND in NB4 (201 µM), HL60 (248 µM) and MOLM13 (124 µM) are presented in Figure 10 B, C and D indicating LND to be more effective after 48 hour treatment in MOLM13 and NB4 cells at lower concentrations than when treated for 24 hours. |
. figure 9.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 9.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 proliferation assay | |
| 细胞系/动物模型 | HL60, MOLM13, NB4, and PBMC cells | |
| 浓度 | 0~1000 µM | |
| 处理时间 | 24 h | |
| 实验结果 | No significant difference (P>0.05) in reduced metabolically active cells was obtained between HL60 and NB4 cells after 24 hour treatment with LND. IC50s of LND was obtained from WST-1 proliferation assay, and are presented in Figure 9B, C and D for HL60 (149 µM), MOLM13 (218 µM) and NB4 (203 µM), respectively. A wider 95% CI is observed for the IC50 of LND in treated NB4 cells (Figure 9D) than for HL60 and MOLM13, thus we cannot exclude the possibility that the IC50 of NB4 could be present anywhere between 106 – 387 µM. |
. figure 7.jpg) |
数据来源 | Uinversity of Bergen thesis (2016). Figure 7.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2) |
| 方法 | WST-1 assay | |
| 细胞系/动物模型 | NB4 cells | |
| 浓度 | 12.5, 25, 50, 75 and 100 µM | |
| 处理时间 | 48 h | |
| 实验结果 | The combined effect of HU and MMF, shown in Figure 7A, followed the same anti-proliferative response to that of MMF alone and no additive effect or synergism was achieved. As both HK1 and HPRT1 were down-regulated by VPA in BNML rats, the combination of LND and MMF (Figure 7B) was investigated for potential synergistic or additive effect on proliferation and apoptosis. |
| 分子量 | 321.16 |
| 分子式 | C15H10Cl2N2O2 |
| CAS号 | 50264-69-2 |
| 溶解性（25°C） | DMSO 44 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 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 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
[3] Gong X, et al. Br J Pharmacol. Mechanism of lonidamine inhibition of the CFTR chloride channel.
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