Ivermectin是一种大环内酯类内外抗寄生虫药，对体内和体外寄生虫均有活性。
Cas No.:70288-86-7
Sample solution is provided at 25 µL, 10mM.
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Ivermectin is a macrolide endectocide with activity against both endoparasites and ectoparasites [1]. Ivermectin disrupts neurotransmission in nerve and muscle cells, causing hyperpolarisation of the neuronal membrane, inducing paralysis of somatic muscles, particularly the pharyngeal pump, killing the parasites [2]. Ivermectin has been widely used to inhibit parasitic infections and kill viruses[3].
In vitro, Ivermectin treatment for 48 hours significantly inhibited the proliferation of C6 cells and U251 cells, with IC50 values of 16.32µM and 14.58µM, respectively[4]. 2.5µM of Ivermectin treatment for 72 hours reduced the proliferation of Pseudorabies virus (PRV) in BHK-21 cells and inhibited the entry of PRV DNA polymerase auxiliary subunit UL42 into the cell nucleus[5].
In vivo, Ivermectin treatment via oral administration at a dose of 0.2mg/kg twice a week for 5 weeks significantly increased the expression level of Cyp 3a11 in the liver of mice and the mRNA level of Cyp 1a1 in the intestine [6]. Intraperitoneal injection of a 3mg/kg dose of Ivermectin every other day for 30 days, which significantly inhibited tumor growth in the ovarian cancer xenograft mouse model, without affecting the body weight of the mice[7].
References:
[1] Dourmishev, Assen L., Lyubomir A. Dourmishev, and Robert A. Schwartz. "Ivermectin: pharmacology and application in dermatology." International journal of dermatology 44.12 (2005): 981-988.
[2] Crump A. Ivermectin: enigmatic multifaceted ‘wonder’drug continues to surprise and exceed expectations[J]. The Journal of antibiotics, 2017, 70(5): 495-505.
[3] Johnson-Arbor K. Ivermectin: a mini-review[J]. Clinical Toxicology, 2022, 60(5): 571-575.
[4] Song D, Liang H, Qu B, et al. Ivermectin inhibits the growth of glioma cells by inducing cell cycle arrest and apoptosis in vitro and in vivo[J]. Journal of Cellular Biochemistry, 2019, 120(1): 622-633.
[5] Lv C, Liu W, Wang B, et al. Ivermectin inhibits DNA polymerase UL42 of pseudorabies virus entrance into the nucleus and proliferation of the virus in vitro and vivo[J]. Antiviral research, 2018, 159: 55-62.
[6] Albérich M, Ménez C, Sutra J F, et al. Ivermectin exposure leads to up-regulation of detoxification genes in vitro and in vivo in mice[J]. European journal of pharmacology, 2014, 740: 428-435.
[7] Zhang X, Qin T, Zhu Z, et al. Ivermectin augments the in vitro and in vivo efficacy of cisplatin in epithelial ovarian cancer by suppressing Akt/mTOR signaling[J]. The American journal of the medical sciences, 2020, 359(2): 123-129.
Ivermectin是一种大环内酯类内外抗寄生虫药，对体内和体外寄生虫均有活性[1]。Ivermectin可破坏神经和肌肉细胞中的神经传递，引起神经元膜超极化，诱导体肌（尤其是咽泵）麻痹，从而杀死寄生虫[2]。Ivermectin已被广泛用于抑制寄生虫感染和杀灭病毒[3]。
在体外，Ivermectin处理48小时显著抑制了C6细胞和U251细胞的增殖，IC50值分别为16.32µM和14.58µM[4]。2.5µM的Ivermectin处理BHK-21细胞72小时，降低了c(PRV)的增殖，并抑制了PRV DNA聚合酶辅助亚基UL42进入细胞核[5]。
在体内，每周两次口服0.2mg/kg剂量的Ivermectin，持续5周，显著增加了小鼠肝脏中Cyp 3a11的表达水平以及肠道中Cyp 1a1的mRNA水平[6]。每隔一天腹腔注射3mg/kg剂量的Ivermectin，持续30天，显著抑制了卵巢癌异种移植小鼠模型中的肿瘤生长，且未影响小鼠的体重[7]。
| Cell experiment [1]: | |
Cell lines | C6 cells |
Preparation Method | C6 cells were seeded at a density of 8×103 cells/well in a 96-well plate and cultured in DMEM medium supplemented with 1% fetal bovine serum (FBS) and 1% penicillin and streptomycin for 24h. C6 cells were subsequently treated with different concentrations of Ivermectin (0, 5, 10, 15, and 20µM) for 48h. Cell viability was analyzed. |
Reaction Conditions | 0, 5, 10, 15, and 20µM; 48h |
Applications | Ivermectin treatment significantly reduced the cell viability of C6 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | NOD/SCID mice |
Preparation Method | Ten million PA-1 cells suspended in 100μl of PBS were injected subcutaneously into NOD/SCID mice. After the development of palpable tumors, the mice were randomized into 4 treatment groups (n=10 each group): vehicle control (80%/20% saline/DMSO), Ivermectin at 3mg/kg on alternating days via intraperitoneal injection, cisplatin at 1mg/kg twice per week via intraperitoneal injection. Mice were treated with the drugs for 30 days and then euthanized via CO2 inhalation. Tumor length and width were measured every 3 days, and tumor volume was calculated using the formula: width2×length /2. |
Dosage form | 3mg/kg; every other day for 30 days; i.p. |
Applications | Ivermectin treatment significantly inhibited tumor growth in the PA-1 xenograft mouse model. |
References: | |
| Cas No. | 70288-86-7 | SDF | |
| 别名 | 伊维菌素; MK-933 | ||
| 化学名 | Ro 5-2807 | ||
| Canonical SMILES | C/C([C@@H](O[C@H]1C[C@H](OC)[C@@H](O[C@H]2C[C@H](OC)[C@@H](O)[C@H](C)O2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@@H]4C5=O)=C\C[C@@H]6C[C@H](O5)C[C@@]7(O[C@@]([C@@H](C)CC)([H])[C@@H](C)CC7)O6 | ||
| 分子式 | C48H74O14 | 分子量 | 875.09 |
| 溶解度 | ≥ 43.7545mg/mL in DMSO | 储存条件 | Store at 2-8°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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1427 mL | 5.7137 mL | 11.4274 mL |
| 5 mM | 228.5 μL | 1.1427 mL | 2.2855 mL |
| 10 mM | 114.3 μL | 571.4 μL | 1.1427 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 | ||||||||||
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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，
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2.
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