Emamectin Benzoate (MK-244) 是一种口服有效的神经系统毒物，其通过结合昆虫中的GABA受体发挥作用。Emamectin Benzoate 是阿维菌素 (Avermectin; HY-15311) 的半合成衍生物之一，具有广谱的杀虫和杀螨活性。Emamectin Benzoate 诱导ROS介导的 DNA 损伤和细胞凋亡。Emamectin Benzoate 是 Emamectin B1a benzoate 和 Emamectin B1b benzoate 的混合物，主要成分为 Emamectin B1a benzoate。
| 生物活性 | Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum ofinsecticidaland acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cellapoptosis. Emamectin Benzoate, a mixture of the natural Emamectin B1a benzoate and Emamectin B1b benzoate, has the main component of Emamectin B1a benzoate[1][2]. |
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体外研究
(In Vitro) | Emamectin Benzoate (MK-244; 2.5-40 μM; 12 and 24 h) decreases cell viability in a time- and dose-dependent manner[1].
Emamectin Benzoate (2.5-20 μM; 24 hours) induces apoptosis and DNA damage in 16HBE cells. Emamectin Benzoate induces ROS generation in 16HBE cells[1].
Emamectin Benzoate (2.5-20 μM; 12 hours) increases the amounts of cytochrome-c, caspase-3, cas-pase-9, cleaved-PARP, Bax/Bcl-2[1].
Emamectin Benzoate (2.5, 5, 10, 15 μM; 72 h) inhibits cell viability with an IC50of 3.72 μM in Trichoplusia Tn5B1-4 cell. Emamectin Benzoat induces chromatin condensation in nuclei and cell apoptosis[2].
Cell Viability Assay[1] | Cell Line: | human normal bronchial epithelial cell line 16HBE | | Concentration: | 2.5, 5, 7.5,10,15, 20, 40 μM | | Incubation Time: | 12 and 24 hours | | Result: | Decreased cell viability in a time- and dose-dependent manner wirh IC50s of 11.88 μM and 9.67 μM in 12 and 24 hours, respectively. |
Apoptosis Analysis[1] | Cell Line: | human normal bronchial epithelial cell line 16HBE | | Concentration: | 2.5, 5, 10, 20 μM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis and caused chromatin shrinkage and nuclear fragmentation. |
Western Blot Analysis[1] | Cell Line: | human normal bronchial epithelial cell line 16HBE | | Concentration: | 2.5, 5, 10, 20 μM | | Incubation Time: | 12 hours | | Result: | Increased the amounts of cytochrome-c, caspase-3, cas-pase-9, cleaved-PARP, Bax/Bcl-2. |
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体内研究
(In Vivo) | Emamectin Benzoate (MK-244; oral; 25-100 mg/kg/day; for 14 days) causes a marked induction of oxidative damage in liver tissue[3].
| Animal Model: | 10 weeks old Swiss albino male mice (25-30 g)[3] | | Dosage: | 25, 50, 100 mg/kg | | Administration: | Oral; daily; for 14 days | | Result: | Caused a marked induction of oxidative damage in liver tissue as demonstrated by an increased level of TBARS and reduced GSH level. |
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| 分子量 | 1008.24(Based on Emamectin B1a Benzoate)
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| 中文名称 | 甲胺基阿维菌素苯甲酸盐；因灭汀苯甲酸盐；埃玛菌素苯甲酸盐 |
| 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 : ≥ 31 mg/mL *"≥" means soluble, but saturation unknown. 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 (Infinity mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (Infinity 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (Infinity 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 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: ≥ 2.08 mg/mL (Infinity mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (Infinity 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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