Avermectin B1 (Abamectin) 是阿维菌素 (avermectin) 的两个相似片段的混合物。Avermectin B1 是一种口服抗感染剂，可用于寄生虫、害虫、农牧业的研究。Avermectin B1 还可以诱导 ROS 的产生，并产生细胞毒性 (cytotoxicity)、诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。
| 生物活性 | Avermectin B1 (Abamectin) is a mixture of two similar segments of avermectin. Avermectin B1 is an orallyanti-infectionagent, which can be used in the research of parasitic worms, insect pests, agriculture and animal husbandry. Avermectin B1 can also induce the production of ROS and inducescytotoxicity,apoptosisandautophagy[1][2][4]. |
体外研究
(In Vitro) | Avermectin B1 (0-80 μM, 12 h) induces cytotoxicity through MAPK and ATM/ATR pathway in mouse embryonic fibroblast (MEF) cells, and induces ROS-mediated DNA damage[1].
Avermectin B1 (36 μg/mL, 72 h) has strong nematicidal efect of onG. pallidain aqueous solution, and negatively influences viability and infectivity ofG. pallida J2detected in potato roots(cv. Spunta)[2].
Abamectin (10 μM, 24 h) induces significant cytotoxicity by overproduction of ROS in haemocytes ofErocheir sinensis[3].
Abamectin (4 μM, 24 h) induces apoptosis and autophagy by inhibiting ROS-mediated PI3K/AKT signaling in MGC803 cells[4].
Cell Viability Assay[1] | Cell Line: | Mouse embryonic fibroblast (MEF) cells | | Concentration: | 0, 0.5, 5, 10, 20, 40, 80 μM | | Incubation Time: | 12 h | | Result: | Reduced cell viability with an IC50value of 45.6 μM. |
Western Blot Analysis[3] | Cell Line: | MGC803 cells | | Concentration: | 0-4 μM | | Incubation Time: | 24 h | | Result: | Increased active caspase-3 and expression of Bax/Bcl-2, decreased MMP in a dose-dependent manner. |
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体内研究
(In Vivo) | Avermectin B1 (oral administration, 0.2 mg/kg for a single dose) is highly efficacious against intestinal strongyles andOnchoceramicrofilaria in horses[5].
| Animal Model: | Horses (had a pruritic dermatosis)[5] | | Dosage: | 0.2 mg/kg, a single dose. | | Administration: | Oral administration | | Result: | Decreased in mean strongyle egg counts 14, 28 and 42 d after treatment, and resulted in zero microfilaria counts in all horses 14 d after treatment. |
| Animal Model: | Healthy adult female sheep (Pharmacokinetic assay)[6] | | Dosage: | 0.2 mg/kg | | Administration: | Subcutaneous administration (in the left neck area of each sheep) | | Result: | Pharmacokinetic profiles of Avermectin B1
| Parameters | Mean | | Kcl(/day) | 0.17 | | t1/2cl(day) | 4.36 | | Kab(/day) | 0.24 | | t1/2ab(day) | 3.15 | | Cmax(ng/mL) | 6.24 | | tmax(day) | 4.20 | | AUC(0-27)(ng/day/mL) | 80.2 | | AUC(0-∞)(ng/day/mL) | 84.7 | | MRT (day) | 8.80 |
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| 结构分类 | - Antibiotics
- Macrolide Antibiotics
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : ≥ 247 mg/mL(142.60 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 0.5773 mL | 2.8866 mL | 5.7732 mL | | 5 mM | 0.1155 mL | 0.5773 mL | 1.1546 mL | | 10 mM | 0.0577 mL | 0.2887 mL | 0.5773 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 (sealed storage, away from moisture and light)。-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: 2.5 mg/mL (1.44 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (1.44 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 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: 2.5 mg/mL (1.44 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (1.44 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (1.44 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.44 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 25.0 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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