| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Avermectin B1a targets glutamate-gated chloride channels (GluCls) in nematodes and insects, which are not found in mammals, contributing to its selective toxicity. It also binds to high and low affinity sites on the mammalian GABAA receptor. By binding to these channels, Avermectin B1a increases chloride ion conductance, leading to hyperpolarization of neuronal and muscle cell membranes, causing paralysis and death of parasites. The compound's high affinity for parasite-specific targets contributes to its high efficacy and low mammalian toxicity.
|
|---|---|
| ln Vitro |
[3H]AVM B1a preferentially binds to synaptic membranes in multiple areas of the rat brain. [3H]AVM B1a specific binding to intact monolayers of granule cells rises fast with time of incubation, reaching equilibrium after around 20 minutes at 24°C. Higher doses of [3H]AVM B1a result in much increased nonspecific binding, 60% at 25 nM. Various AVM analogs decrease [3H]AVM B1a binding in intact cerebellar neurons in a concentration-dependent manner. AVM B1a and moxidectin have similar efficacy (IC50 values of 120 and 126 nM, respectively) [3]. AVMB1a-stimulated chloride efflux from mouse brain synaptic vesicles arises from the activation of GABA-insensitive chloride channels, which differs from their previously known effects on GABA-gated chloride channels in mouse brain preparations[4].
In vitro studies have demonstrated that Avermectin B1a is a potent antiparasitic agent effective against a wide range of nematodes, mites, and insects. The compound binds to glutamate-gated chloride channels, causing paralysis of parasites without causing hypercontraction or flaccid paralysis. Its mechanism of action is well characterized, and the compound has been extensively studied in vitro using various parasite models. Avermectin B1a is also studied for its binding to mammalian GABAA receptors. |
| ln Vivo |
In soil, fungi are less affected by AVM B1a concentrations beyond 83.3 mg/kg, but bacteria are strongly inhibited by them. High concentrations of AVM B1a, which vary according on the type of soil, also prevent soil respiration. After treating soil earthworms for 7 and 14 days in artificial soil, the half lethal dosage (LD50) of AVM B1a is calculated to be 4.63 mg × cm2 in a filter paper contact test and 24.13 and 17.06 mg/kg, respectively[1]. The LC50 of AVM B1a on earthworms in artificial soil is 17.1 mg/kg for 14 days and 24.1 mg/kg for 7 days, respectively. In two groups exposed to AVM B1a-free soil, almost 80.0% and 94.8%, respectively, of the accumulated AVM B1a are destroyed after one day; nevertheless, earthworms retain traces of AVM B1a for a considerable amount of time[2].
In vivo, Avermectin B1a is widely used as an antiparasitic agent in veterinary and agricultural applications. It is effective against a wide range of internal and external parasites, including nematodes, mites, and insects. The compound is known for its high efficacy and low mammalian toxicity. It is utilized in livestock, companion animals, and crop protection. Avermectin B1a is also used as a research tool to study glutamate-gated chloride channel function and parasite physiology. |
| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for Avermectin B1a typically involve radioligand binding studies using [³H]Avermectin B1a to assess binding to glutamate-gated chloride channels or GABAA receptors. Membrane preparations from parasites or mammalian tissues are incubated with radiolabeled Avermectin B1a, and binding affinity (Kd) and receptor density (Bmax) are determined from saturation binding experiments. Competition binding assays are performed with unlabeled compounds to determine IC₅₀ and Ki values.
|
| Cell Assay |
In vitro cell-based assays for Avermectin B1a use parasite cultures (e.g., nematode larvae, mite cultures) to evaluate antiparasitic activity. Parasites are incubated with Avermectin B1a at various concentrations, and parameters such as motility, viability, and mortality are assessed microscopically. EC₅₀ values are calculated from dose-response curves. Electrophysiological studies using patch-clamp or two-electrode voltage clamp can be performed to assess the compound's effects on chloride channel function in Xenopus oocytes expressing parasite GluCl channels.
|
| Animal Protocol |
In vivo animal studies for Avermectin B1a employ rodent models of parasitic infection or livestock animals naturally infected with parasites. The compound is administered orally, topically, or by injection, and parameters assessed include parasite burden (fecal egg count reduction, worm counts at necropsy), clinical signs of infection, weight gain, and overall health. Safety and tolerability are also evaluated. Avermectin B1a has been extensively validated in these models.
|
| ADME/Pharmacokinetics |
Avermectin B1a has a molecular weight of 873.08 g/mol and a molecular formula of C₄₈H₇₂O₁₄. It is also known as Abamectin B1a, 5-O-Demethylavermectin A1a, and Antibiotic C 076B1a. The compound is a macrocyclic lactone disaccharide with high lipophilicity. It is poorly soluble in water but soluble in organic solvents. Following administration, Avermectin B1a is absorbed and distributed to tissues, metabolized in the liver, and excreted in feces. Its half-life varies depending on the species and route of administration.
|
| Toxicity/Toxicokinetics |
Toxicity Summary
It has low solubility in water and exhibits broad non-specific binding capacity. It can open GABA-insensitive chloride ion channels, reduce membrane resistance, and increase inward conductivity. (T10) Avermectin B1a has low mammalian toxicity due to its selective binding to parasite-specific glutamate-gated chloride channels. However, at high doses, it can cause neurotoxicity in mammals due to binding to GABAA receptors. Side effects may include central nervous system depression, ataxia, and tremors. The compound is classified as a veterinary and agricultural agent and is not intended for human therapeutic use. Comprehensive toxicological data are available from regulatory submissions. |
| References |
|
| Additional Infomation |
Avermectin B1a is an avermectin compound. It has been reported to be found in both Streptomyces avermitilis and Saccharomyces cerevisiae, with available data. Avermectins are a series of macrolide derivatives with potent anthelmintic activity. In recent years, oral or parenteral administration of avermectins has become a common treatment method. These macrolides are produced by fermentation of the soil microorganism Streptomyces avermitilis in carefully prepared laboratory culture media. They are active against a variety of livestock nematodes and arthropod parasites at doses of 300 μg/kg or lower. Unlike macrolides or polyene antibiotics, they lack significant antibacterial or antifungal activity. (L829) See also: Avermectin B1B (related compound).
Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent and the major component of the avermectin family. It is also known as Abamectin B1a. The compound is a potent antiparasitic agent used in veterinary and agricultural applications to control nematodes, mites, and insects. It works by binding to glutamate-gated chloride channels and GABAA receptors. Known for its high efficacy and low mammalian toxicity, it is widely utilized in livestock, companion animals, and crop protection. Not approved for human therapeutic use. |
| Molecular Formula |
C48H72O14
|
|---|---|
| Molecular Weight |
873.09
|
| Exact Mass |
872.492
|
| CAS # |
65195-55-3
|
| PubChem CID |
6434889
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
940.9±65.0 °C at 760 mmHg
|
| Melting Point |
157-162ºC
|
| Flash Point |
268.1±27.8 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.571
|
| LogP |
6.51
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
62
|
| Complexity |
1730
|
| Defined Atom Stereocenter Count |
20
|
| SMILES |
CC[C@H](C)[C@@H]1[C@H](C=C[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
|
| InChi Key |
RRZXIRBKKLTSOM-XPNPUAGNSA-N
|
| InChi Code |
InChI=1S/C48H72O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38/h12-15,17-19,25-26,28,30-31,33-45,49-50,52H,11,16,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+/m0/s1
|
| Chemical Name |
(1'R,2R,3S,4'S,6S,8'R,10'E,12'S,13'S,14'E,16'E,20'R,21'R,24'S)-2-[(2S)-butan-2-yl]-21',24'-dihydroxy-12'-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-3,11',13',22'-tetramethylspiro[2,3-dihydropyran-6,6'-3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene]-2'-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~28.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.86 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 25.0 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: ≥ 2.5 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1454 mL | 5.7268 mL | 11.4536 mL | |
| 5 mM | 0.2291 mL | 1.1454 mL | 2.2907 mL | |
| 10 mM | 0.1145 mL | 0.5727 mL | 1.1454 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
