Spinosad is a bioneurotoxic insecticide with a broader spectrum of action, a blend of spinosyns A and D, which is a fermentation product of soil actinomycetes. Spinosad targets nicotinic acetylcholine receptors (nAChRs) in the insect nervous system. Spinosad has an excellent environmental and mammalian toxicology profile. Has larvae-killing activity.

Physicochemical Properties

Molecular Formula	C83H132N2O20
Molecular Weight	1477.94
Exact Mass	733.512
CAS #	168316-95-8
Related CAS #	Spinosyn A;131929-60-7;Spinosyn D;131929-63-0
PubChem CID	17754356
Appearance	White to off-white solid powder
Density	1.1±0.1 g/cm3
Boiling Point	776.3±60.0 °C at 760 mmHg
Melting Point	84ºC to 99.5ºC
Flash Point	423.3±32.9 °C
Vapour Pressure	0.0±2.7 mmHg at 25°C
Index of Refraction	1.527
LogP	4.86
Hydrogen Bond Acceptor Count	22
Rotatable Bond Count	18
Heavy Atom Count	105
Complexity	2620
Defined Atom Stereocenter Count	34
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)

Biological Activity

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]. 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]. 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]. 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]. Properties, toxicity and current applications of the biolarvicide spinosad. J Toxicol Environ Health B Crit Rev. 2020;23(1):13-26. [6]. Organic insecticide spinosad causes in vivo oxidative effects in the brain of Oreochromis niloticus. Environ Toxicol. 2014;29(3):253-260.

Solubility Data

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. 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. 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 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	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.