| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| Other Sizes |
| Targets |
Target: Ca2+ ATPase[1]
|
|---|---|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
The first step in the biotransformation of cyhalothrin is ester hydrolysis, which yields a 3-phenoxy-4-fluorobenzyl alcohol intermediate and a permethrin acid component. Following ester hydrolysis, 3-phenoxy-4-fluorobenzyl alcohol is partially oxidized to the free metabolite 3-phenoxy-4-fluorobenzoic acid. This metabolite can combine with glycine to form 3-phenoxy-4-fluorohippuric acid, or be hydroxylated to form 4'-hydroxy-3-phenoxy-4-fluorobenzoic acid. The metabolites, along with small amounts of unmetabolized compounds, are excreted in urine and feces. (L857, A562) |
| Toxicity/Toxicokinetics |
Toxicity Summary
Both type I and type II pyrethroids exert their effects by prolonging the opening time of sodium ion channels during nerve cell excitation. They appear to bind to membrane lipids near sodium ion channels, thereby altering channel dynamics. This blocks the closing of sodium ion channels in the nerve, thus prolonging the time it takes for the membrane potential to return to its resting state. Repetitive (sensory, motor) neuronal firing and the prolonged negative afterpotential produce effects very similar to DDT, leading to nervous system hyperactivity, which may result in paralysis and/or death. Other mechanisms of action of pyrethroids include antagonizing γ-aminobutyric acid (GABA)-mediated inhibition, regulating nicotinic cholinergic transmission, enhancing norepinephrine release, and acting on calcium ions. They also inhibit calcium ion channels and Ca2+,Mg2+-ATPase. (T10, T18, L857) Toxicity Data LD50: 869-1271 mg/kg (oral, rat) (L862) LD50: 291-609 mg/kg (oral, mouse) (L862) L50: > 5000 mg/kg (dermal, rat) (L862) |
| References | |
| Additional Infomation |
See also: Cyfluthrin (note moved to).
|
| Molecular Formula |
C22H18CL2FNO3
|
|---|---|
| Molecular Weight |
434.287627696991
|
| Exact Mass |
433.064
|
| CAS # |
1820573-27-0
|
| Related CAS # |
Cyfluthrin;68359-37-5
|
| PubChem CID |
56608859
|
| Appearance |
White to off-white solid powder
|
| LogP |
6.2
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
679
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
Cl/C(=C\C1[C@H](C(=O)O[C@@H](C#N)C2C=CC(=C(C=2)OC2C=CC=CC=2)F)C1(C)C)/Cl
|
| InChi Key |
QQODLKZGRKWIFG-RUTXASTPSA-N
|
| InChi Code |
InChI=1S/C22H18Cl2FNO3/c1-22(2)15(11-19(23)24)20(22)21(27)29-18(12-26)13-8-9-16(25)17(10-13)28-14-6-4-3-5-7-14/h3-11,15,18,20H,1-2H3/t15?,18-,20+/m0/s1
|
| Chemical Name |
[(R)-cyano-(4-fluoro-3-phenoxyphenyl)methyl] (1S)-3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropane-1-carboxylate
|
| 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: 50 mg/mL (115.13 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.76 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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 2: ≥ 2.5 mg/mL (5.76 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 | 2.3026 mL | 11.5130 mL | 23.0261 mL | |
| 5 mM | 0.4605 mL | 2.3026 mL | 4.6052 mL | |
| 10 mM | 0.2303 mL | 1.1513 mL | 2.3026 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.
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