Rotigotine (Synonyms: N-0923; (-)-N 0437)

Name: Rotigotine
Brand: MedChemExpress
SKU: HY-75502
Rating: 4.5 (1 reviews)

Cat. No.: HY-75502 Purity: 99.99% ee.: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

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

Rotigotine Chemical Structure

CAS No. : 99755-59-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 61	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 336	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rotigotine:

1 Publications Citing Use of MCE Rotigotine

•Clin Chem. 2019 Dec;65(12):1522-1531. [Abstract]

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View All Dopamine Receptor Isoform Specific Products:

View All Isoforms

Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

View All Adrenergic Receptor Isoform Specific Products:

View All Isoforms

α adrenergic receptor β adrenergic receptor

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[4]

D₃ Receptor

0.71 nM (Ki)

D₂ Receptor

4-15 nM (Ki)

D₅ Receptor

4-15 nM (Ki)

D₄ Receptor

4-15 nM (Ki)

D₁ Receptor

83 nM (Ki)

5-HT_1A Receptor

30 nM (Ki)

5-HT₇ Receptor

86 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.7 nM Compound: Rotigotine	Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins	[PMID: 24296012]
CHO	EC₅₀	28 nM Compound: Rotigotine	Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins	[PMID: 24296012]
HEK-293T	EC₅₀	3.2 nM Compound: Rotigotine	Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding	[PMID: 28489379]
HEK-293T	EC₅₀	4.1 nM Compound: Rotigotine	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]
HEK-293T	EC₅₀	4.4 nM Compound: Rotigotine	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]

In Vitro

Rotigotine (0.01-10 µM) slightly protects dopaminergic neurons against MPP⁺ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone^[2].

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

In Vivo

Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect^[3].

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

Animal Model:	Male Sprague–Dawley rats^[3]
Dosage:	0.1, 0.5, 1, and 5 mg/kg
Administration:	Subcutaneous injection; for 14 days.
Result:	Had antidepressant effect at a dose of 1 mg/kg or less.

Clinical Trial

Molecular Weight

315.47

Formula

C₁₉H₂₅NOS

CAS No.

99755-59-6

Appearance

Solid

Color

Off-white to pink

SMILES

CCCN(CCC1=CC=CS1)[C@H]2CCC3=C(C=CC=C3O)C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (158.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1699 mL	15.8494 mL	31.6987 mL
5 mM	0.6340 mL	3.1699 mL	6.3397 mL
10 mM	0.3170 mL	1.5849 mL	3.1699 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (7.92 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 (7.92 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 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 (7.92 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). 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 Corn oil, and mix evenly.

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).

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: 99.99% ee.: 99.98%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (248 KB) RP-HPLC (348 KB) NP-HPLC (300 KB)

Handling Instructions (2659 KB)

References

[1]. Wood M, et, al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35. [Content Brief]

[2]. Radad K, et, al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP⁺ and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86. [Content Brief]

[3]. Bertaina-Anglade V, et, al. Antidepressant properties of rotigotine in experimental models of depression. Eur J Pharmacol. 2006 Oct 24;548(1-3):106-14. [Content Brief]

[4]. Scheller D, et, al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.1699 mL	15.8494 mL	31.6987 mL	79.2468 mL
	5 mM	0.6340 mL	3.1699 mL	6.3397 mL	15.8494 mL
	10 mM	0.3170 mL	1.5849 mL	3.1699 mL	7.9247 mL
	15 mM	0.2113 mL	1.0566 mL	2.1132 mL	5.2831 mL
	20 mM	0.1585 mL	0.7925 mL	1.5849 mL	3.9623 mL
	25 mM	0.1268 mL	0.6340 mL	1.2679 mL	3.1699 mL
	30 mM	0.1057 mL	0.5283 mL	1.0566 mL	2.6416 mL
	40 mM	0.0792 mL	0.3962 mL	0.7925 mL	1.9812 mL
	50 mM	0.0634 mL	0.3170 mL	0.6340 mL	1.5849 mL
	60 mM	0.0528 mL	0.2642 mL	0.5283 mL	1.3208 mL
	80 mM	0.0396 mL	0.1981 mL	0.3962 mL	0.9906 mL
	100 mM	0.0317 mL	0.1585 mL	0.3170 mL	0.7925 mL

Rotigotine Related Classifications

Neurological Disease Endocrinology

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:

Rotigotine99755-59-6N-0923 (-)-N 0437N0923N 0923Dopamine ReceptorAdrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine Receptordopaminereceptor5-HT1Aα2B-adrenergicInhibitorinhibitorinhibit

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Rotigotine (Synonyms: N-0923; (-)-N 0437)

Customer Review

Other Forms of Rotigotine:

Rotigotine Related Antibodies

1 Publications Citing Use of MCE Rotigotine

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dopamine Receptor Isoform Specific Products:

View All Adrenergic Receptor Isoform Specific Products:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Rotigotine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rotigotine Related Classifications

Keywords:

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