Lonidamine
(Synonyms: 氯尼达明; AF-1890; Diclondazolic Acid; DICA) 目录号 : GC11532
Lonidamine是一种己糖激酶、线粒体丙酮酸载体（在分离的大鼠肝脏线粒体中Ki为2.5μM）和质膜单羧酸转运蛋白抑制剂，同时还抑制线粒体复合物 II。
Cas No.:50264-69-2
Sample solution is provided at 25 µL, 10mM.
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Lonidamine is an inhibitor of hexokinase, mitochondrial pyruvate carrier (with a Ki of 2.5μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporter, and also inhibits mitochondrial complex II [1]. Lonidamine is an anti-tumor drug that can inhibit aerobic glycolysis in cancer cells [2]. Lonidamine can be used in the research of mitochondrial metabolism and inflammation [3].
In vitro, Lonidamine (3, 10, and 30μM; 24h) treatment of IL-4, IL-13, and TNF-α-induced human nasal mucosal epithelial cells significantly and dose-dependently reduced the expression of CXCL1 and PTN, confirming its direct anti-inflammatory and anti-resorptive effects on nasal epithelial cells [4]. Lonidamine (150μM; 45min and 3h) treatment of human melanoma DB-1 cells significantly reduced NADH levels, the Fp redox ratio (Fp/(NADH + Fp)) increased, and mitochondrial redox capacity significantly decreased [5].
In vivo, Lonidamine (100mg/kg; ip) treatment for 2 hours significantly reduced the βNTP level in nude mice with DB-1 human melanoma. At the same time, the NTP levels in DB-1, HCC1806, BT-474, A2780 and LNCaP also decreased respectively [6]. Lonidamine (1, 3, and 10mg/kg/day for 11 days; i.g.) treatment alleviated the symptoms of chronic sinusitis mice, reduced sneezing, cytokine release, inflammatory cell infiltration, and goblet cell hyperplasia. Lonidamine inhibits inflammation by inhibiting the differentiation of inflammatory epithelial cells and neutrophils through Cxcl1-Cxcr2 [4].
References:
[1] Shutkov IA, Okulova YN, Tyurin VY, et al. Ru(III) Complexes with Lonidamine-Modified Ligands. Int J Mol Sci. 2021;22(24):13468.
[2] Nancolas B, et al. The anti-tumour agent lonidamine is a potent inhibitor of the mitochondrial pyruvate carrier and plasma membrane monocarboxylate transporters. Biochem J. 2016 Apr 1;473(7):929-36.
[3] Xueqian Yin, et al. Hexokinase 2 couples glycolysis with the profibrotic actions of TGF-β. Sci Signal. 2019 Dec 17;12(612):eaax4067.
[4] Liu J, Wu L, Wei H, et al. Lonidamine alleviates inflammation and tissue remodeling in a mouse model of eosinophilic chronic sinusitis: A single-cell transcriptomics study[J]. International Immunopharmacology, 2025, 163: 115258.
[5] Xu H N, Feng M, Nath K, et al. Optical redox imaging of lonidamine treatment response of melanoma cells and xenografts[J]. Molecular Imaging and Biology, 2019, 21(3): 426-435.
[6] Nath K, Nelson D S, Heitjan D F, et al. Lonidamine induces intracellular tumor acidification and ATP depletion in breast, prostate and ovarian cancer xenografts and potentiates response to doxorubicin[J]. NMR in Biomedicine, 2015, 28(3): 281-290.
Lonidamine是一种己糖激酶、线粒体丙酮酸载体（在分离的大鼠肝脏线粒体中Ki为2.5μM）和质膜单羧酸转运蛋白抑制剂，同时还抑制线粒体复合物 II [1]。Lonidamine是一种抗肿瘤药物，可抑制癌细胞中的有氧糖酵解 [2]。Lonidamine可用于线粒体代谢和炎症的研究 [3]。
在体外，Lonidamine（3, 10和30μM; 24h）处理IL-4、IL-13和TNF-α诱导的人鼻黏膜上皮细胞，显著且剂量依赖性地降低了CXCL1和PTN的表达，证实了其对鼻上皮细胞的直接抗炎和抗重塑作用 [4]。Lonidamine（150μM; 45min和3h）处理人黑色素瘤DB-1细胞，显著降低了NADH水平，Fp氧化还原比（Fp/（NADH+Fp））增加，线粒体氧化还原能力显著降低 [5]。
在体内，Lonidamine（100mg/kg; ip）治疗2小时显著降低了裸鼠DB-1人黑色素瘤的βNTP水平，同时DB-1、HCC1806、BT-474、A2780和LNCaP的NTP的水平也分别下降 [6]。Lonidamine（1, 3和10mg/kg/day; i.g.）治疗11天缓解了慢性鼻窦炎小鼠的症状，减少了打喷嚏、细胞因子释放、炎症细胞浸润以及杯状细胞增生。Lonidamine通过Cxcl1-Cxcr2抑制炎症上皮细胞和嗜中性粒细胞的分化来抑制炎症 [4]。
| Cell experiment [1]: | |
Cell lines | DB-1 cell |
Preparation Method | For testing Lonidamine treatment response of cultured cells, DB-1 cells were expanded in phenol-red free RPMI 1640 complete medium. Suspended DB-1 cells (4 × 104, 200μl) were transferred to a 35-mm glass bottom dish (MatTek, MA) and incubated for 4h to allow cells to attach to the glass surface. Fresh medium (1 ml) was then added, and the dish was incubated for 20h. Approximately 1h before imaging, the medium was removed and the dish were rinsed twice with PBS (with Ca2+ and Mg2+) followed by adding 1ml live cell imaging solution (LCIS) spiked with 11mM glucose and 2mM glutamine. For the Lonidamine-treated group, the cells were treated with 150μM Lonidamine for 45min (0.8% or 0.2% DMSO in the glucose and glutamine-spiked LCIS). The control group was treated with 0.8% or 0.2% DMSO for 45min. |
Reaction Conditions | 150μM; 45min |
Applications | Lonidamine significantly reduced the NADH level in the cells, and the Fp redox ratio (Fp/(NADH + Fp)) increased, while the mitochondrial redox capacity was significantly decreased. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were housed in ventilated cages. All animal experiments were approved by the institutional animal care and use committee at the Zhejiang University Laboratory Animal Center. A mouse model of eosinophilic chronic sinusitis (ECRS) was established using intranasal papain administration (20μg in 20μL PBS) on Days 0–2 and 7–10 for a total of 7 doses, with controls receiving PBS. Treatment groups included gavage with Lonidamine (1, 3, or 10mg/kg), or intraperitoneal DEX (1mg/kg) daily for 11 days. Seventy-two mice (balanced for sex) were divided into six groups (n = 12 per group): control, ECRS, ECRS+ Lonidamine (1, 3, or 10mg/kg), and ECRS+DEX. No adverse effects were noted. Mice were anesthetized with isoflurane and euthanized using CO2 (30% vol/min). This study followed ethical guidelines for humane animal treatment. |
Dosage form | 1, 3, and 10mg/kg/day for 11 days; i.g. |
Applications | Lonidamine alleviated ECRS symptoms, reducing sneezing, cytokine release, inflammatory cell infiltration, and goblet cell hyperplasia. |
References: | |
| Cas No. | 50264-69-2 | SDF | |
| 别名 | 氯尼达明; AF-1890; Diclondazolic Acid; DICA | ||
| 化学名 | 1-[(2,4-dichlorophenyl)methyl]indazole-3-carboxylic acid | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O | ||
| 分子式 | C15H10Cl2N2O2 | 分子量 | 321.16 |
| 溶解度 | ≥ 11.1mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
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