Referencia número: HY-75502

Rotigotine

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

3 Cited Publications

Revisión del cliente

Based on 3 publication(s) in Google Scholar

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.

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Pureza: 99.90%
No. CAS: 99755-59-6
Fòrmula: C₁₉H₂₅NOS
Peso molecular:315.47

Almacenamiento:

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

Rotigotine Chemical Structure

No. CAS: 99755-59-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (3)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]^[4]

D₃ Receptor

0.71 nM (Ki)

5-HT_1A Receptor

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)

Ver todos los productos específicos de isoformas Dopamine Receptor :

Ver todos los productos específicos de isoformas Adrenergic Receptor :

Ver todos los productos específicos de isoformas 5-HT Receptor :

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 99755-59-6
Appearance Solid
Peso molecular 315.47
Fòrmula C₁₉H₂₅NOS
Color Off-white to pink
SMILES

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

N-0923; (-)-N 0437
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (3)

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Journal Impact Factor

Acta Pharmacol Sin

Dysfunction of subthalamic dopaminergic circuitry contributes to anxiety- and depression-like behaviors in 6-OHDA lesion-induced hemiparkinsonian mice. [Abstract]

2025 May 6. PMID: 40329003
Clin Chem

Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]

2019 Dec;65(12):1522-1531. PMID: 31578215
bioRxiv

Go/z-biased coupling profile of the dopamine D3 receptor. [Abstract]

2025 Aug 12:2025.08.08.668522. PMID: 40832361

Solvente y solubilidad

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Rotigotine

3 Cited Publications

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Rotigotine

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Publications Citing Use of MedChemExpress (MCE) Rotigotine

Ver todos los productos específicos de isoformas Dopamine Receptor

Ver todos los productos específicos de isoformas Adrenergic Receptor

Ver todos los productos específicos de isoformas 5-HT Receptor

Actividad biológica

Chemical Information

Publications (3)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Rotigotine Related Classifications

HY-75502 Related Classifications