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Rotenone [83-79-4]

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Référence NB-64-18580-1mL

Conditionnement : 1mLx10mM(inDMSO)

Marque : Neo Biotech

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Rotenone

(Synonyms: Rotocide, Rotenon, Paraderil, Dactinol, Barbasco) Copy Product Info

Synonyms: Rotocide, Rotenon, Paraderil, Dactinol, Barbasco

Catalog No. T2970 Copy Product Info

Purity: 99.88%

Rotenone is a natural plant-derived insecticide that acts as an inhibitor of mitochondrial electron transport chain complex I. It promotes the generation of mitochondrial reactive oxygen species, induces apoptosis, and is commonly used to establish Parkinson's disease models.

Cas No. 83-79-4

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.88%

Color:White to Yellow

Product Introduction

Bioactivity

Description	Rotenone is a natural plant-derived insecticide that acts as an inhibitor of mitochondrial electron transport chain complex I. It promotes the generation of mitochondrial reactive oxygen species, induces apoptosis, and is commonly used to establish Parkinson's disease models.
Targets & IC50	697 cells (72 h):0.3 μM, A549 cells (24 h):26 μM (ED50), A549 cells:0.04 μg/mL, A549 cells:0.901 μg/mL, 697 cells (48 h):0.3 μM
In vitro	METHODS: Human leukemia cells HL-60 were treated with Rotenone (0-1000 nM) for 30 min and oxygen consumption was measured using a Clark oxygen electrode. RESULTS: Rotenone dose-dependently inhibited HL-60 cell respiration. Rotenone inhibited cellular respiration by more than 96% at 500 nM. [1] METHODS: 10th DIV cells were treated with Rotenone (20 nM) for 48 h. LDH levels were measured by LDH release assay. RESULTS: LDH release can be used as an indicator of general cytotoxicity. rotenone induced an increase in LDH release, and LDH activity increased more than 6-fold compared to the control group. LDH activity increased more than 6-fold compared to the control group.[2]
In vivo	METHODS: To establish a reproducible mouse model of Rotenone-induced Parkinson's disease (PD), Rotenone (2.5 mg/kg) was administered intraperitoneally to C57Bl/6 mice once daily for two weeks. RESULTS: Systemic exposure of mice to Rotenone resulted in progressive accumulation and regional spread of p129 aggregates, which preceded the maximal loss of DAn. [3] METHODS: To study neurotoxicity, Rotenone (30-100 mg/kg) was administered orally to C57BL/6 mice once daily for fifty-six days. RESULTS: The survival of Rotenone-treated mice at 30 mg/kg was unchanged from 28-56 days, although the survival of Rotenone-treated mice was reduced to approximately 70% within one week. 100 mg/kg Rotenone-treated mice showed a sudden decrease in survival after 28 days, and ultimately to approximately 15% after 56 days. A regimen of Rotenone given chronically at 30 mg/kg for 56 days is more useful for understanding the mechanisms of DA neurodegeneration. [4]
Synonyms	Rotocide, Rotenon, Paraderil, Dactinol, Barbasco
Disease Modeling Protocol	Parkinson's Disease (PD) Model Modeling Mechanism： Rotenone, as an inhibitor of mitochondrial complex I, induces PD pathology through multiple mechanisms: ① It selectively inhibits the activity of mitochondrial complex I in dopaminergic neurons of the substantia nigra pars compacta (SNc), reducing ATP production and causing structural damage such as mitochondrial swelling and cristae breakage; ② It promotes the excessive production of reactive oxygen species (ROS), inducing oxidative stress and damaging lipids, proteins, and DNA; ③ It activates the apoptosis pathway, upregulating the expression of the pro-apoptotic protein Bax and downregulating the expression of the anti-apoptotic protein Bcl-XL, leading to the death of SNc dopaminergic neurons; ④ It inhibits the activity of vesicular monoamine transporter 2 (VMAT2), increasing cytoplasmic dopamine accumulation and exacerbating neurotoxicity. Related Products： Rotenone (T2970) Modeling Method： Experimental Subject： Rats: Wistar strain, male, 6 weeks old, body weight 200–250 g Dosage and Administration Route： ① Core modelling: Rotenone (2 mg/kg/day) dissolved in soybean oil administered subcutaneously (SC); ② Control treatment: equal volume soybean oil administered via same route; ③ Intervention validation (optional): Edaravone (10 mg/kg/day) dissolved in physiological saline, administered intraperitoneally (IP) in two divided doses (7:00 am and 7:00 pm), initiated concurrently with modelling and continued for 5 weeks Dosing Frequency and Duration Model： Rotenone injection once daily for 5 weeks Validation： Behavioral indicators: Motor function: 81% (22/27 animals) of the model group showed typical PD symptoms (kyphosis, stiffness, bradykinesia), and the fall latency in the grid test and bar test was significantly prolonged (P<0.05 vs control group); edaravone intervention could shorten the latency by more than 85%; Pathological indicators: Neuronal damage: SNc tyrosine hydroxylase (TH) positive neurons decreased by 60.48%, and striatum (CPu) TH immunostaining intensity decreased by 65.67%; edaravone intervention could salvage 44.66% of dopaminergic neurons; Mitochondrial damage: Transmission electron microscopy showed mitochondrial swelling, cristae breakage, and vacuolar degeneration in SNc neurons; edaravone intervention could significantly improve mitochondrial structure; Molecular indicators: Oxidative stress: Midbrain ROS levels were significantly increased; edaravone could inhibit 73.35% of ROS generation; Apoptosis-related: Bax protein expression was upregulated, Bcl-XL... Downregulation of expression can be reversed by edaravone; Transporter expression: VMAT2 mRNA and protein levels are reduced, and edaravone can upregulate their expression by 45%-70%. Precautions： After the behavioral test, the rats were euthanized and their midbrains were micro-perforated. Intracellular ROS levels were then measured. References：Xiong N,et,al. Edaravone guards dopamine neurons in a rotenone model for Parkinson's disease. PLoS One. 2011;6(6):e20677.

Chemical Properties

Molecular Weight	394.42
Formula	C₂₃H₂₂O₆
Cas No.	83-79-4
Smiles	O=C1C=2C(=C3C(O[C@@H](C(C)=C)C3)=CC2)O[C@]4([C@@]1(C=5C(OC4)=CC(OC)=C(OC)C5)19)19
Relative Density.	1.27(20°C)

Storage & Solubility Information

Storage

Keep away from direct sunlight,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (253.54 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.95 mg/mL (10.01 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5354 mL	12.6768 mL	25.3537 mL	126.7684 mL
5 mM	0.5071 mL	2.5354 mL	5.0707 mL	25.3537 mL
10 mM	0.2535 mL	1.2677 mL	2.5354 mL	12.6768 mL
20 mM	0.1268 mL	0.6338 mL	1.2677 mL	6.3384 mL
50 mM	0.0507 mL	0.2535 mL	0.5071 mL	2.5354 mL
100 mM	0.0254 mL	0.1268 mL	0.2535 mL	1.2677 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Rotenonep53NAPDHMitochondrialMetabolismMitochondrial MetabolismInhibitorinhibitAutophagyApoptosis

Related Tags: Rotenone chemical structure | Rotenone in vivo | Rotenone in vitro | Rotenone formula | Rotenone molecular weight