Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
500mg |
|
||
Other Sizes |
|
ln Vitro |
By attaching to nicotinic acetylcholine receptors (nAChRs), the archetypal unit that functions as a neurotransmitter ligand-gated ion channel, spinosad binds to acetylcholine (Ach) and acts as an allosteric agonist of Ach [4].
|
---|---|
ln Vivo |
The pedicidal tetracyclic macrolides Spinosad A and Spinosad D are naturally occurring together to form Spinosad. 0.9% Spinosad predominantly disrupts nicotinic acetylcholine receptors in insects, causing neuronal excitation that, after sustained overexcitation, causes lice to become paralyzed owing to neuromuscular fatigue. Both permethrin-sensitive and -resistant lice populations are eliminated with spinosad 0.9%. Moreover, it possesses ovicidal qualities that cause lice and their eggs to die [5]. In vivo oxidation is induced in the Nile tilapia brain by spinosad. Spinosad increases GSH/GSSG, Hsp70, tGSH, and GPx activities while decreasing the ratio of GSH/GSSG and GPx activities. It also causes glutathione reductase activity to be induced. Spinosad alters the characteristics of the GSH-related antioxidant system and Hsp70, which results in oxidative effects on brain tissue [6].
|
References |
[1]. Duchet C, et al. Effects of Bacillus thuringiensis israelensis and spinosad on adult emergence of the non-biting midges Polypedilum nubifer (Skuse) and Tanytarsus curticornis Kieffer (Diptera: Chironomidae) in coastal wetlands. Ecotoxicol Environ Saf. 2015;115:272-278.
[2]. Wang J, et al. A three amino acid deletion in the transmembrane domain of the nicotinic acetylcholine receptor α6 subunit confers high-level resistance to spinosad in Plutella xylostella. Insect Biochem Mol Biol. 2016;71:29-36. [3]. Huang J, et al. High Level of Spinosad Production in the Heterologous Host Saccharopolyspora erythraea. Appl Environ Microbiol. 2016;82(18):5603-5611. Published 2016 Aug 30. [4]. McCormack PL. Spinosad: in pediculosis capitis. Am J Clin Dermatol. 2011;12(5):349-353. [5]. Santos VSV, et al. Properties, toxicity and current applications of the biolarvicide spinosad. J Toxicol Environ Health B Crit Rev. 2020;23(1):13-26. [6]. Piner P, et al. Organic insecticide spinosad causes in vivo oxidative effects in the brain of Oreochromis niloticus. Environ Toxicol. 2014;29(3):253-260. |
Molecular Formula |
C83H132N2O20
|
---|---|
Molecular Weight |
1477.94
|
CAS # |
168316-95-8
|
Related CAS # |
Spinosyn A;131929-60-7;Spinosyn D;131929-63-0
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
CC[C@H]1CCC[C@@H]([C@@H](C)C(=O)C2=C[C@@H]3[C@H](C=C[C@@H]4C[C@H](C[C@H]43)O[C@H]5[C@@H]([C@@H]([C@H]([C@H](C)O5)OC)OC)OC)C2CC(=O)O1)O[C@H]6CC[C@@H]([C@@H](C)O6)N(C)C
|
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: 10 mg/mL (6.77 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (0.68 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: 1 mg/mL (0.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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: ≥ 1 mg/mL (0.68 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 | 0.6766 mL | 3.3831 mL | 6.7662 mL | |
5 mM | 0.1353 mL | 0.6766 mL | 1.3532 mL | |
10 mM | 0.0677 mL | 0.3383 mL | 0.6766 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.