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| Other Sizes |
| ln Vitro |
Avermectin B1 (0 - 80 μM, 12 h) causes ROS-mediated DNA damage and cytotoxicity in murine fibroblasts (MEFs) through ATM/ATR and MAPK [1]. Avermectin B1 (10 μM, 24 h) causes a considerable amount of cytotoxicity by causing ROS overproduction in Chinese mitten crab hemocytes. G.pallida is toxically killed by /mL, 72 h) [2]. In MGC803 cells, avermectin B1 (4 μM, 24 h) inhibits ROS-mediated PI3K/AKT signal fluorescence, hence inducing autophagy and cell fluorescence [4].
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| ln Vivo |
Avermectin B1 (powder coating, 0.2 mg/kg single dosage) works wonders against Onchocera microfilariae and Strongyloides equine [5].
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| Cell Assay |
Cell viability assay [1]
Cell Types: mouse embryonic fibroblasts [3]. (MEF) Cell Tested Concentrations: 0, 0.5, 5, 10, 20, 40, 80 μM Incubation Duration: 12 hrs (hours) Experimental Results: Cell viability diminished, IC50 value was 45.6 μM. Western Blot Analysis [3] Cell Types: MGC803 Cell Tested Concentrations: 0-4 μM Incubation Duration: 24 h Experimental Results: The expression of active caspase-3 and Bax/Bcl-2 increased, and MMP diminished in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Horse (with pruritic skin disease) [5]
Doses: 0.2 mg/kg, single dose. Route of Administration: Oral Experimental Results: Mean Strongyloides egg counts were diminished at 14, 28 and 42 days after treatment, and all horses had zero microfilariae counts after 14 days of treatment. Animal/Disease Models: Healthy adult ewes (pharmacokinetic/PK/PK determination) [6] Doses: 0.2 mg/kg Route of Administration: subcutaneous injection (left neck of each sheep) Experimental Results: pharmacokinetic/PK/PK characteristics of abamectin B1 Parameter average 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 |
| References |
[1]. Yiran Liang, et al. Abamectin induces cytotoxicity via the ROS, JNK, and ATM/ATR pathways. PLoS One. Environ Sci Pollut Res Int. 2020 Apr;27(12):13726-13734.
[2]. Nicola Sasanelli, et al. Abamectin Efficacy on the Potato Cyst Nematode Globodera pallida. Plants (Basel). 2019 Dec 19;9(1):12. [3]. Yi Huang, et al. Cytotoxicity induced by abamectin exposure in haemocytes of Chinese mitten crab, Eriocheir sinensis. Environ Toxicol Pharmacol. 2020 Jul;77:103384. [4]. Shanshan Zhu, et al. Abamectin induces apoptosis and autophagy by inhibiting reactive oxygen species-mediated PI3K/AKT signaling in MGC803 cells. J Biochem Mol Toxicol. 2019 Jul;33(7):e22336. [5]. Mogg TD, et al. Efficacy of avermectin B1 given orally against equine intestinal strongyles and Onchocera microfilaria. Aust Vet J. 1990 Nov;67(11):399-401. [6]. Peyami Sari, et al. Pharmacokinetics of Abamectin/Levamisole Combination in a Medium Chain Mono and Diglyceride-Based Vehicle and an In Vitro Release and In Vitro In Vivo Correlation Study for Levamisole. AAPS PharmSciTech. 2017 May;18(4):1254-1260. |
| Molecular Formula |
C95H142O28
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|---|---|
| Molecular Weight |
1732.15
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| Exact Mass |
1730.9688
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| CAS # |
71751-41-2
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
940.9±65.0 °C at 760 mmHg
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| Melting Point |
150-155°C
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| Flash Point |
268.1±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.571
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| LogP |
6.51
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| SMILES |
C[C@@H](CC)[C@]1([H])[C@@H](C)C=C[C@@]2(O[C@@]3([H])C[C@]([H])(OC([C@@]4([H])[C@@](/C(CO5)=C/C=C/[C@H](C)[C@H](O[C@@]6([H])C[C@H](OC)[C@@H](O[C@]7([H])O[C@@H](C)[C@H](O)[C@@H](OC)C7)[C@H](C)O6)/C(C)=C/C3)(O)[C@@]5([H])[C@H](O)C(C)=C4)=O)C2)O1.C[C@H]8C=C[C@@]9(O[C@@]%10([H])C[C@]([H])(OC([C@@]%11([H])[C@@](/C(CO%12)=C/C=C/[C@H](C)[C@H](O[C@@]%13([H])C[C@H](OC)[C@@H](O[C@]%14([H])O[C@@H](C)[C@H](O)[C@@H](OC)C%14)[C@H](C)O%13)/C(C)=C/C%10)(O)[C@@]%12([H])[C@H](O)C(C)=C%11)=O)C9)O[C@@H]8C(C)C
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| Chemical Name |
Avermectin B(sub 1)
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| Synonyms |
Abamectin AgrimekAvidAvid ECAffirmAgri-MekEPA Pesticide Chemical Code 122804MK 0936MK 936VertimecZephyrHSDB 6941Avomec
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~286.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (2.38 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02533336 | TERMINATED | Drug: abamectin and fenpyroximate | Malaria | National Institute for Medical Research, Tanzania | 2015-11-09 | Phase 3 |
| NCT01869205 | COMPLETED | Device: Endobronchial valve | Pulmonary Emphysema | Asan Medical Center | 2013-03 | Phase 3 |
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