| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Avermectin B1a, a macrocyclic lactone disaccharide compound, is an anthelmintic and antiparasitic agent. It acts by binding to high and low affinity sites on the mammalian GABAA receptor.
| 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].
|
|---|---|
| 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].
|
| Toxicity/Toxicokinetics |
Toxicity Summary
It has low solubility in water and extensive non-specific binding. It opens GABA-insensitive chloride channels, reducing membrane resistance and increasing conductance inward. (T10) |
| References |
|
| Additional Infomation |
Avermectin B1a is an avermectin.
Abamectin B1a has been reported in Streptomyces avermitilis and Saccharomyces cerevisiae with data available. The avermectins are a series of macrocyclic lactone derivatives with potent anthelmintic properties. A commonly used therapy in recent times has been based on oral or parenteral administration of avermectins, which are macrocyclic lactones produced by fermentation of various, carefully prepared laboratory broths using the soil micro-organism Streptomyces avermitilis. They show activity against a broad range of nematodes and arthropod parasites of domestic animals at dose rates of 300 microgram/kg or less. Unlike the macrolide or polyene antibiotics, they lack significant antibacterial or antifungal activity. (L829) See also: Abamectin B1B (related). |
| 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
