| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g | |||
| 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].
|
| 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. |
| 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. |
| 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 |
112-123 °C
|
| 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 Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
22
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
105
|
| Complexity |
2620
|
| Defined Atom Stereocenter Count |
34
|
| 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
|
| InChi Key |
JFLRKDZMHNBDQS-SGSTVUCESA-N
|
| 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
|
| 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
|
| 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.
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
Copyright 2020 InvivoChem LLC | All Rights Reserved
