Rotenone

Name: Rotenone
Brand: MedChemExpress
SKU: HY-B1756
Rating: 5.0 (81 reviews)

Cat. No.: HY-B1756 Purity: 99.74%: FAQs
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Rotenone is a mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

For research use only. We do not sell to patients.

Rotenone Chemical Structure

CAS No. : 83-79-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
1 g	USD 60	In-stock	Estimated Time of Arrival: December 31
5 g	USD 108	In-stock	Estimated Time of Arrival: December 31
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50 g		Get quote

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Based on 81 publication(s) in Google Scholar

Other Forms of Rotenone:

Rotenone (Standard) Get quote

80 Publications Citing Use of MCE Rotenone

: Rotenone purchased from MedChemExpress. Usage Cited in: Mediat Inflamm. 2020 Aug 17;2020:3934769. [Abstract]; Western blot analysis of NLRP3, IL-1β, IL-18, and caspase-1 p10 expression in renal tubular epithelial cells stimulated with Rotenone. Rotenone induces NLRP3 inflammasome activation.

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Description

Rotenone is a mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

Cellular Effect

Cell Line	Type	Value	Description	References
697	IC₅₀	0.3 μM Compound: 8	Cytotoxicity against human 697 cells after 48 hrs by MTS assay Cytotoxicity against human 697 cells after 48 hrs by MTS assay	[PMID: 23895019]
697	IC₅₀	0.3 μM Compound: 8	Cytotoxicity against human 697 cells after 72 hrs by MTS assay Cytotoxicity against human 697 cells after 72 hrs by MTS assay	[PMID: 23895019]
A549	IC₅₀	0.04 μg/mL Compound: 3	Cytotoxicity against human A549 cells after 3 days by SRB assay Cytotoxicity against human A549 cells after 3 days by SRB assay	[PMID: 16562843]
A549	IC₅₀	0.901 μg/mL Compound: 1	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 22204911]
A549	ED₅₀	26 μM Compound: rotenone	Antitumor activity against human A549 cells after 24 hrs by MTT assay Antitumor activity against human A549 cells after 24 hrs by MTT assay	[PMID: 17482824]
BC1 cell line	ED₅₀	0.039 μg/mL Compound: 1	Cytotoxicity against human BC1 cells after 72 hrs Cytotoxicity against human BC1 cells after 72 hrs	[PMID: 2614425]
Col2	ED₅₀	0.15 μg/mL Compound: 1	Cytotoxicity against human Col2 cells after 72 hrs Cytotoxicity against human Col2 cells after 72 hrs	[PMID: 2614425]
DU-145	IC₅₀	0.465 μg/mL Compound: 1	Cytotoxicity against human DU145 cells by SRB assay Cytotoxicity against human DU145 cells by SRB assay	[PMID: 22204911]
HCT-116	IC₅₀	0.045 ug Compound: 5	Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting	[PMID: 21452840]
HeLa	IC₅₀	78 μM Compound: Rotenone	Cytotoxicity against human HeLa cells after 24 hrs by luminometry Cytotoxicity against human HeLa cells after 24 hrs by luminometry	[PMID: 21741837]
HepG2	IC₅₀	1.52 μM Compound: Rotenone	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 30613327]
HepG2	ED₅₀	15 μM Compound: rotenone	Antitumor activity against human HepG2 cells after 24 hrs by MTT assay Antitumor activity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 17482824]
HT-1080	ED₅₀	0.047 μg/mL Compound: 1	Cytotoxicity against human HT1080 cells after 48 hrs Cytotoxicity against human HT1080 cells after 48 hrs	[PMID: 2614425]
HT-29	IC₅₀	0.3 μM Compound: 8	Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay	[PMID: 23895019]
HT-29	ED₅₀	202 μM Compound: rotenone	Antitumor activity against human HT29 cells after 24 hrs by MTT assay Antitumor activity against human HT29 cells after 24 hrs by MTT assay	[PMID: 17482824]
KB	ED₅₀	0.067 μg/mL Compound: 1	Cytotoxicity against human KB cells after 72 hrs Cytotoxicity against human KB cells after 72 hrs	[PMID: 2614425]
KB	IC₅₀	0.513 μg/mL Compound: 1	Cytotoxicity against human KB cells by SRB assay Cytotoxicity against human KB cells by SRB assay	[PMID: 22204911]
L5178Y	IC₅₀	0.3 μM Compound: 30	Cytotoxicity against mouse L5178Y cells by MTT assay Cytotoxicity against mouse L5178Y cells by MTT assay	[PMID: 28075580]
MCF7	IC₅₀	0.008 μg/mL Compound: 3	Cytotoxicity against human MCF7 cells after 3 days by SRB assay Cytotoxicity against human MCF7 cells after 3 days by SRB assay	[PMID: 16562843]
MCF7	ED₅₀	161 μM Compound: rotenone	Antitumor activity against human MCF7 cells after 24 hrs by MTT assay Antitumor activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 17482824]
MES-SA	ED₅₀	147 μM Compound: rotenone	Antitumor activity against human MES-SA cells after 24 hrs by MTT assay Antitumor activity against human MES-SA cells after 24 hrs by MTT assay	[PMID: 17482824]
MES-SA/Dx5	ED₅₀	214 μM Compound: rotenone	Antitumor activity against doxorubucin-resistant human MES-SA/Dx5 cells by MTT assay after 24 hrs Antitumor activity against doxorubucin-resistant human MES-SA/Dx5 cells by MTT assay after 24 hrs	[PMID: 17482824]
P388	ED₅₀	0.005 μg/mL Compound: 1	Cytotoxicity against mouse P388 cells after 48 hrs Cytotoxicity against mouse P388 cells after 48 hrs	[PMID: 2614425]
Raji	IC₅₀	1.1 μM Compound: 8	Cytotoxicity against human Raji cells after 72 hrs by MTS assay Cytotoxicity against human Raji cells after 72 hrs by MTS assay	[PMID: 23895019]
Raji	IC₅₀	4.2 μM Compound: 8	Cytotoxicity against human Raji cells after 48 hrs by MTS assay Cytotoxicity against human Raji cells after 48 hrs by MTS assay	[PMID: 23895019]
SH-SY5Y	IC₅₀	74.1 μM Compound: Rotenone	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 27689727]
SK-MEL-2	ED₅₀	0.092 μg/mL Compound: 1	Cytotoxicity against human SK-MEL-2 cells after 72 hrs Cytotoxicity against human SK-MEL-2 cells after 72 hrs	[PMID: 2614425]
U-937	IC₅₀	0.07 μM Compound: 3	Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay	[PMID: 17158054]
U-937	IC₅₀	0.2 μM Compound: 3	Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay	[PMID: 17158054]
U-937	IC₅₀	13 μM Compound: 3	Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay	[PMID: 17158054]

In Vitro

Mitogen Activated Protein Kinase (MAPK), Toll-like receptor, Wnt, and Ras signaling pathways are intensively involved in the effect of rotenone on the ENS^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rotenone can be used to create Parkinson's disease models.

Induction of Parkinson's model^[6]

Background

Cell loss of dopaminergic (DA) neurons in the substantia nigra is a common feature of Parkinson's disease. Rotenone induces DA neuronal cytotoxicity, leading to motor deficits in the substantia nigra and loss of DA neuronal cells in mice.

Specific Mmodeling Methods

Mice: male • C57BL/6J mice • 8 weeks old • 20-25 g
Administration: 30 mg/kg in 12 mL/kg • po • once daily for 28 days

Note

The control group was treated with 0.5% Carboxylmethylcellulose (CMC).

Modeling Indicators

Mouse dyskinesia: slow movement/inadequate movement ability.

Correlated Product(s): /

Opposite Product(s): /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

394.42

Formula

C₂₃H₂₂O₆

CAS No.

83-79-4

Appearance

Solid

Color

White to light yellow

SMILES

O=C1[C@]2([H])[C@](COC3=CC(OC)=C(OC)C=C32)([H])OC4=C5C(O[C@@H](C(C)=C)C5)=CC=C14

Structure Classification

Flavonoids

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (126.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5354 mL	12.6768 mL	25.3537 mL
5 mM	0.5071 mL	2.5354 mL	5.0707 mL
10 mM	0.2535 mL	1.2677 mL	2.5354 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 25 mg/mL (63.38 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (281 KB) SDS (623 KB)

COA (253 KB) HNMR (263 KB) RP-HPLC (226 KB) LCMS (93 KB) OR (256 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Khadrawy YA, et al. Cerebellar neurochemical and histopathological changes in rat model of Parkinson's disease induced by intrastriatal injection of rotenone. Gen Physiol Biophys. 2016 Nov 30. [Content Brief]

[2]. Guan Q, et al. RNA-Seq Expression Analysis of Enteric Neuron Cells with Rotenone Treatment and Prediction of Regulated Pathways. Neurochem Res. 2016 Nov 30. [Content Brief]

[3]. Kishore Kumar SN, et al. Morinda citrifolia mitigates rotenone-induced striatal neuronal loss in male Sprague-Dawley rats by preventing mitochondrial pathway of intrinsic apoptosis. Redox Rep. 2016 Nov 24:1-12. [Content Brief]

[4]. Zhang ZN, et al. Subcutaneous rotenone rat model of Parkinson's disease: dose exploration study. Brain Res. 2016 Nov 19. pii: S0006-8993(16)30776-4. [Content Brief]

[5]. Li N, et al. Mitochondrial complex I inhibitor rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production. J Biol Chem. 2003 Mar 7;278(10):8516-25. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5354 mL	12.6768 mL	25.3537 mL	63.3842 mL
	5 mM	0.5071 mL	2.5354 mL	5.0707 mL	12.6768 mL
	10 mM	0.2535 mL	1.2677 mL	2.5354 mL	6.3384 mL
	15 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2256 mL
	20 mM	0.1268 mL	0.6338 mL	1.2677 mL	3.1692 mL
	25 mM	0.1014 mL	0.5071 mL	1.0141 mL	2.5354 mL
	30 mM	0.0845 mL	0.4226 mL	0.8451 mL	2.1128 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5846 mL
	50 mM	0.0507 mL	0.2535 mL	0.5071 mL	1.2677 mL
	60 mM	0.0423 mL	0.2113 mL	0.4226 mL	1.0564 mL
	80 mM	0.0317 mL	0.1585 mL	0.3169 mL	0.7923 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rotenone83-79-4Mitochondrial MetabolismAutophagyApoptosisInhibitorinhibitorinhibit

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