| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Nicotinic acetylcholine receptors (nAChRs) and GABA receptors in insects. Spinosyn A and D have the highest level of insecticidal activity and act as allosteric modulators of insect nAChRs. The Spinosyns do not have antibiotic effects on bacteria or fungi. The exact binding site on insect nAChRs is distinct from that of neonicotinoids.
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| 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].
Spinosad acts on the insect nervous system by activating nicotinic acetylcholine receptors (nAChRs) and modulating GABA receptors, leading to hyperexcitation, paralysis, and death. It exhibits no significant activity on mammalian nAChRs, contributing to its favorable mammalian safety profile. In vitro assays demonstrate potent insecticidal activity with LC50 values in the low ppm range against target insect species. |
| 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].
Spinosad exhibits excellent insecticidal efficacy in vivo against a wide range of agricultural pests, including caterpillars, leafminers, thrips, and fruit flies. It also shows activity against insect pests of stored grain. Spinosad is effective at low application rates (20-100 g active ingredient per hectare) and provides rapid knockdown and long residual activity. The insecticide is considered safe for beneficial insects, including bees (when dry), predatory insects, and mammals. |
| Enzyme Assay |
Cell-free assays for Spinosad are not typically used because it is an insecticide with a defined target in insects. For receptor binding studies using insect membrane preparations (e.g., head homogenates of fruit flies (Drosophila melanogaster) or cockroaches (Periplaneta americana)), membranes (50-200 microg protein) are incubated with radiolabeled imidacloprid (a neonicotinoid, 0.5-2 nM) or radiolabeled alpha-bungarotoxin and varying concentrations of spinosyn A or D (0.1-10000 nM) in 50 mM Tris-HCl buffer pH 7.4 for 60-120 minutes at room temperature. Non-specific binding is determined in the presence of 10 microM unlabeled imidacloprid or 1 mM nicotine. Bound radioligand is separated by rapid filtration through GF/B filters, and radioactivity is measured by liquid scintillation or gamma counting. Spinosad acts as an allosteric modulator with a binding site distinct from the orthosteric site. Alternatively, voltage-sensitive ion flux assays using insect synaptoneurosomes can be performed: synaptoneurosomes are incubated with spinosad (0.01-100 microM) in the presence of radiolabeled ions (22Na+ or ⁸⁶Rb+), and ion influx is measured by rapid filtration and scintillation counting. Spinosad activates insect nAChRs, enhancing 22Na+ influx. For enzyme activity assays, spinosad does not significantly inhibit acetylcholinesterase, monoamine oxidase, or other mammalian enzymes at insecticidal concentrations.
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| Cell Assay |
For cellular assays, insect cell lines such as Drosophila Schneider 2 (S2) cells or Spodoptera frugiperda Sf9 cells (expressing native or recombinant insect nAChR subunits) are seeded in 96-well plates (50,000-100,000 cells/well) in appropriate insect cell culture medium (Schneider's medium or SF-900) supplemented with 10% FBS for 24-48 hours. For calcium mobilization assays, cells are loaded with Fluo-4 AM (2.5 microM) in HBSS buffer (for insect cells, pH adjusted to 6.8-7.0) for 60 minutes at 27degC. Spinosad (0.01-100 microM) is added, and fluorescence is measured. For whole-cell patch-clamp electrophysiology, cells are voltage-clamped at -60 to -80 mV, and spinosad is applied via rapid perfusion to measure agonist-induced inward currents. Spinosad is an allosteric activator of insect nAChRs, showing effects at low microM concentrations. For cell viability assays, Sf9 or S2 cells are treated with spinosad (0.01-100 microM) for 24-72 hours, and viability is measured by MTT or CellTiter-Glo. Spinosad has low toxicity to insect cell lines at insecticidal concentrations due to the absence of the intact insect nervous system. For mammalian cell control assays (HEK-293 or CHO cells expressing mammalian nAChR subunits), spinosad (up to 100 microM) shows no significant activity, confirming its insect-selectivity. EC50 for insect nAChR activation is typically in the 0.1-10 microM range.
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| Animal Protocol |
For insecticidal activity assays, target insect species (e.g., Spodoptera exigua (beet armyworm) or Plutella xylostella (diamondback moth)) are used. For topical application: 2-4 microL of spinosad solution in acetone or water with a surfactant (0.01-0.1% Triton X-100) is applied to the dorsal thorax of anesthetized insects (CO2 or cold anesthesia). Concentrations range from 0.1-10000 ppm (0.0001-10%). 10-30 insects per concentration are treated. Insects are placed in ventilated containers with appropriate food (artificial diet or host plant leaves) and maintained at 25+/-1degC, 16:8 light-dark cycle, 60+/-5% relative humidity. Mortality is recorded at 24, 48, and 72 hours post-treatment. Insects are considered dead if they cannot right themselves when turned over. LC50 and LC90 values are calculated by probit analysis using software (e.g., PoloPlus, SPSS). Positive controls: a commercial insecticide (e.g., deltamethrin, chlorpyrifos). For leaf dip assay: plant leaves (e.g., cabbage, cotton) are cut into discs (2-3 cm diameter) and dipped into spinosad solutions (0.1-10000 ppm) for 10-30 seconds. Leaves are air-dried for 1-2 hours, then placed in petri dishes with 5-10 larvae per dish. Mortality is recorded at 24, 48, and 72 hours. For contact assay: insects are placed in glass vials or plastic cups coated with spinosad solutions (0.5-2 mL, dried to form a residue). For ingestion assay: spinosad is incorporated into artificial diet at 0.1-1000 ppm. For field trials: spinosad is applied at 20-100 g active ingredient per hectare using standard spray equipment. Insect counts are conducted pre-treatment and at 1, 3, 5, 7, 14 days post-treatment. Percent control is calculated using Abbott's formula: % control = [(1 - (T after / T before)) / (1 - (C after / C before))] × 100, where T = treated, C = control. LC50 values for spinosad range from 0.5-10 ppm depending on insect species and application method. For non-target species testing (e.g., bees, beneficial insects, fish, birds), specialized protocols follow OECD or EPA guidelines. Spinosad is considered safe for beneficial insects when residues are dry.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Topically applied medication is not absorbed. Topically applied medication is not distributed. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use During Lactation Currently, there is no clinical information regarding the use of echinococcine during lactation. Since echinococcine is not absorbed systemically after topical application, it will not enter breast milk. However, the topical suspension contains benzyl alcohol, which may be absorbed systemically through the skin. High doses of benzyl alcohol may be toxic to newborns, but are unlikely to enter breast milk. Any product applied to the breast should be washed off with soap and water before breastfeeding to avoid direct contact with the infant. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Protein Binding When applied topically, it does not bind to plasma proteins. Spinosad (mixture of spinosyn A and spinosyn D, CAS 168316-95-8) is a natural product insecticide with low mammalian toxicity. In rats, oral LD50 >5000 mg/kg, dermal LD50 >5000 mg/kg, inhalation LC50 >5 mg/L, indicating low acute toxicity. Spinosad is rapidly absorbed and eliminated with a half-life of 1-2 days in mammals. It is metabolized by hepatic microsomal enzymes (CYP450) and excreted in urine and feces (80% within 5 days). Spinosad has low bioaccumulation potential. In the environment, spinosad degrades rapidly via photolysis (half-life 1-2 days on leaf surfaces) and microbial degradation in soil (half-life 9-17 days). It has low groundwater contamination potential due to high soil binding (Koc). In plants, spinosad is metabolized to spinosyns A and D, with residues primarily on surfaces. Spinosad is not volatile (low vapor pressure). For human exposure, spinosad has Acceptable Daily Intake (ADI) of 0-0.02 mg/kg bw/day. No adverse effects were observed in chronic studies in mammals, including no carcinogenicity, genotoxicity, or reproductive toxicity. |
| References | |
| Additional Infomation |
Spinosad is a liceicide composed of spinosad A and spinosad D (in approximately a 5:1 ratio) for the topical treatment of head lice in children (4 years and older) and adults. Spinosad is an insecticide based on compounds isolated from *Saccharopolyspora spinosa*. Spinosad has also been used to treat flea infestations in cats and against KS1 type *Ctenocephalides felis* fleas in dogs. Numerous studies have also explored its use in other animals and crops. Spinosad is a liceicide. A combination of spinosad A and D; isolated from *Saccharopolyspora spinosa*. See also: milbemime; spinosad (component).
Drug Indication Echinocandins are indicated for the treatment of head lice infestations in adults and children aged 6 months and older, and for the treatment of scabies in adults and children aged 4 years and older. FDA Label Mechanism of Action Spinosad is a mixture of echinomycin A and echinomycin D in a 5:1 ratio. This combination primarily works by altering nicotine acetylcholine receptors, causing neuronal hyperexcitability, ultimately leading to paralysis and death of the lice. Pharmacodynamics Spinosad has a novel mechanism of action similar to that of GABA antagonists. Echinocandin A also has slightly higher biological activity than echinosad D. Spinosad is classified by the EPA and WHO as a reduced-risk pesticide with low toxicity to mammals and the environment. It has been approved for use in organic agriculture in many countries. Spinosad is not a drug and has no approved human therapeutic indications. Common trade names include Spinosad, Entrust, Conserve, Success, and Tracer. It is used in agriculture (fruits, vegetables, cotton, corn), public health (mosquito control), and veterinary medicine (flea and tick control for pets). CAS number: 168316-95-8. For research and commercial use as an insecticide; not for human medicinal use. |
| Molecular Formula |
C83H132N2O20
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|---|---|
| Molecular Weight |
1477.94
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| Exact Mass |
733.512
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| CAS # |
168316-95-8
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| Related CAS # |
Spinosyn A;131929-60-7;Spinosyn D;131929-63-0
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| PubChem CID |
17754356
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
776.3±60.0 °C at 760 mmHg
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| Melting Point |
112-123 °C
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| Flash Point |
423.3±32.9 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.527
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| LogP |
4.86
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
105
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| Complexity |
2620
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| Defined Atom Stereocenter Count |
34
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| SMILES |
CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C=C[C@H]3[C@@H]2CC(=O)O1)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C.CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C(=C[C@H]3[C@@H]2CC(=O)O1)C)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C
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| InChi Key |
JFLRKDZMHNBDQS-SGSTVUCESA-N
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| InChi Code |
InChI=1S/C42H67NO10.C41H65NO10/c1-11-26-13-12-14-35(53-37-16-15-34(43(6)7)24(4)49-37)23(3)38(45)33-20-31-29(32(33)21-36(44)51-26)17-22(2)28-18-27(19-30(28)31)52-42-41(48-10)40(47-9)39(46-8)25(5)50-42;1-10-26-12-11-13-34(52-36-17-16-33(42(5)6)23(3)48-36)22(2)37(44)32-20-30-28(31(32)21-35(43)50-26)15-14-25-18-27(19-29(25)30)51-41-40(47-9)39(46-8)38(45-7)24(4)49-41/h17,20,23-32,34-35,37,39-42H,11-16,18-19,21H2,1-10H3;14-15,20,22-31,33-34,36,38-41H,10-13,16-19,21H2,1-9H3/t23-,24-,25+,26+,27-,28+,29-,30-,31-,32+,34+,35+,37+,39+,40-,41-,42+;22-,23-,24+,25-,26+,27-,28-,29-,30-,31+,33+,34+,36+,38+,39-,40-,41+/m11/s1
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| Chemical Name |
(1S,2S,5R,7S,9S,10S,14R,15S,19S)-15-[(2R,5S,6R)-5-(dimethylamino)-6-methyloxan-2-yl]oxy-19-ethyl-4,14-dimethyl-7-[(2R,3R,4R,5S,6S)-3,4,5-trimethoxy-6-methyloxan-2-yl]oxy-20-oxatetracyclo[10.10.0.02,10.05,9]docosa-3,11-diene-13,21-dione;(1S,2R,5S,7R,9R,10S,14R,15S,19S)-15-[(2R,5S,6R)-5-(dimethylamino)-6-methyloxan-2-yl]oxy-19-ethyl-14-methyl-7-[(2R,3R,4R,5S,6S)-3,4,5-trimethoxy-6-methyloxan-2-yl]oxy-20-oxatetracyclo[10.10.0.02,10.05,9]docosa-3,11-diene-13,21-dione
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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 |
| 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: 10 mg/mL (6.77 mM)
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| 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05310734
Conditions:ScabiesLink: https://clinicaltrials.gov/ct2/show/NCT01660321
Conditions:PediculosisLink: https://clinicaltrials.gov/ct2/show/NCT00545753
Conditions:Pediculosis
Title:Safety and Efficacy Study of NatrOVA Creme Rinse - 1% and NIX Creme Rinse in Subjects 6 Months or Older With Head Lice
Status:Completed
updateDate:2012-10-11
Ctid:NCT00545168
Link: https://clinicaltrials.gov/ct2/show/NCT00545168
Conditions:Pediculus Capitis InfestationLink: https://clinicaltrials.gov/ct2/show/NCT00591331
Conditions:Head LiceProducts are for research use only; We do not sell to patients
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