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| Targets |
Fenpropathrin acts on voltage-gated sodium channels in nerve cell membranes. By prolonging the opening time of sodium channels during nerve cell excitation, it causes sustained depolarization, repetitive neuronal firing, and eventual paralysis of insects. This mechanism makes it effective against a broad spectrum of agricultural pests.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Fenpropathrin is used as a research tool to study pyrethroid-induced neurotoxicity. In vitro, fenpropathrin exposure increases sodium channel open time in cultured neurons, leading to altered firing patterns and calcium dysregulation. It may induce dopaminergic cell injury at high concentrations, making it valuable for Parkinson's disease research models. |
| ln Vivo |
In vivo, fenpropathrin is used to create animal models of Parkinson's disease. Administration in rodents induces progressive parkinsonian symptoms including motor deficits and dopaminergic neuron degeneration. The compound exhibits potent insecticidal activity in agricultural pest species with rapid onset of paralysis and mortality following contact or ingestion.
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| Enzyme Assay |
For receptor-binding assays, incubate purified sodium channels or synaptosomal membranes with tritiated fenpropathrin or its d5 analog at concentrations ranging from 1 nM to 10 uM in binding buffer (50 mM Tris-HCl, pH 7.4) for 60 minutes at 25degC. Separate bound from free ligand by rapid filtration through glass fiber filters and quantify by scintillation counting or LC-MS for d5.
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| Cell Assay |
Culture primary rat cortical neurons or dopaminergic neuronal cell lines (e.g., SH-SY5Y) in appropriate growth medium. Treat cells with fenpropathrin-d5 at concentrations ranging from 1-100 uM for 12-48 hours. Assess cell viability by MTT or LDH assays, measure reactive oxygen species (ROS) by DCFH-DA staining, and evaluate apoptosis by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
For Parkinson's disease modeling, administer fenpropathrin to adult male C57BL/6 mice via intraperitoneal injection at doses of 1-5 mg/kg daily for 7-28 days. Monitor motor function using rotarod and open field tests weekly. After the treatment period, sacrifice animals and collect brain tissues (striatum and substantia nigra) for immunohistochemical staining of tyrosine hydroxylase to assess dopaminergic neuron loss.
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| ADME/Pharmacokinetics |
As a deuterated internal standard, fenpropathrin-d5 is not typically studied for its own PK. However, unlabeled fenpropathrin is rapidly absorbed after oral exposure in mammals, with peak plasma concentrations within 1-4 hours. It is extensively metabolized by ester hydrolysis and oxidation, with a terminal half-life of approximately 12-24 hours. The d5 analog is expected to have similar PK profiles.
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| Toxicity/Toxicokinetics |
Fenpropathrin exhibits moderate acute toxicity in mammals, with oral LD50 values ranging from 50-200 mg/kg in rodents. Chronic exposure may induce neurobehavioral changes and dopaminergic neurodegeneration, making it a model for environmental toxin-induced parkinsonism. It shows low dermal absorption and is classified as moderately hazardous by WHO. Cardiotoxic effects including altered heart rate have been observed in zebrafish models.
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| References | |
| Additional Infomation |
Fenpropathrin-d5 is primarily used as an analytical standard for quantifying fenpropathrin residues in environmental and agricultural samples using GC-MS/MS or LC-MS/MS methods. The deuterium label provides superior stability and minimal isotope effects during mass spectrometric analysis. Fenpropathrin is banned or restricted in some countries due to environmental persistence and neurotoxicity concerns.
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| Molecular Formula |
C22H18D5NO3
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| Molecular Weight |
354.45
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| Related CAS # |
Fenpropathrin;39515-41-8
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| Appearance |
White to off-white solid powder
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8213 mL | 14.1064 mL | 28.2127 mL | |
| 5 mM | 0.5643 mL | 2.8213 mL | 5.6425 mL | |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8213 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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