| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Rotigotine Hydrochloride (N-0437; N-0923) is a potent, non-selective and dopamine receptor full agonist, used in the treatment of Parkinson's disease and restless legs syndrome. Rotigotine is an agonist of the dopamine D2 and D3 receptors, with corresponding Ki values of 13 and 0.71 nM for D2 and D3. Additionally, rotigotine exhibits a strong affinity for adrenergic α2B and 5-HT1A receptors.
| Targets |
D3 Receptor ( Ki = 0.71 nM ); D2 Receptor ( Ki = 4-15 nM ); D5 Receptor ( Ki = 4-15 nM ); D4 Receptor ( Ki = 4-15 nM ); D1 Receptor ( Ki = 83 nM ); α1A ( Ki = 176 nM ); α1B ( IC50 = 273 nM ); α2A ( IC50 = 338 nM ); α2B ( IC50 = 27 nM ); 5-HT1A Receptor ( Ki = 30 nM ); 5-HT7 Receptor ( Ki = 86 nM )
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| Enzyme Assay |
In 96-well polypropylene tubes, binding assays are carried out with a final volume of 2 mL for D1 and D4 membranes and 1 mL for D2, D3, and D5 membranes. These tubes contain the following materials: 50 μL radioligand, 10 μL drug/buffer/non-specific binding, buffer (final concentration 50 mM Tris-HCl pH 7.4, MgCl2 2 mM), and membranes (5 μg protein for D2 and D3 and 25 μg protein for D1 and D5). Rapid vacuum filtration through A/C glass fiber filters presoaked in 0.1% polyethylenimine is used to determine bound radioligand after 120 minutes of incubation at 25°C. Liquid scintillation counting is used to determine the retained radioactivity after the filters are four times cleaned with 2 mL of ice-cold ishing buffer (Tris-HCl 50 mM, pH 7.4 at 4°C).
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| References |
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| Molecular Formula |
C19H26CLNOS
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| Molecular Weight |
351.93
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| Exact Mass |
351.14
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| Elemental Analysis |
C, 64.84; H, 7.45; Cl, 10.07; N, 3.98; O, 4.55; S, 9.11
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| CAS # |
125572-93-2
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| Related CAS # |
Rotigotine; 99755-59-6; Rotigotine-d7 hydrochloride
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| Appearance |
Solid powder
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| SMILES |
CCCN(CCC1=CC=CS1)[C@H]2CCC3=C(C2)C=CC=C3O.Cl
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| InChi Key |
CEXBONHIOKGWNU-NTISSMGPSA-N
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| InChi Code |
InChI=1S/C19H25NOS.ClH/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21;/h3-7,13,16,21H,2,8-12,14H2,1H3;1H/t16-;/m0./s1
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| Chemical Name |
(6S)-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol;hydrochloride
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| Synonyms |
Rotigotine Hydrochloride; N 0923; N-0923; N-0924; Rotigotine HCl; Neupro
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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 |
| 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) |
DMSO: ≥ 50 mg/mL (~142.1 mM)
H2O: ~4.8 mg/mL (~13.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8415 mL | 14.2074 mL | 28.4147 mL | |
| 5 mM | 0.5683 mL | 2.8415 mL | 5.6829 mL | |
| 10 mM | 0.2841 mL | 1.4207 mL | 2.8415 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00296192 | Completed | Drug: Rotigotine nasal spray Drug: Placebo |
Parkinson's Disease | UCB Pharma | February 2006 | Phase 2 |
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Products are for research use only; We do not sell to patients
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