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Rotigotine-

Catalog No. T6647Cas No. 99755-59-6
Alias SPM 962, Neupro, N-0923, N-0437

Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.

Rotigotine-

Rotigotine-

Purity: 99.76%
Catalog No. T6647Alias SPM 962, Neupro, N-0923, N-0437Cas No. 99755-59-6
Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.
Pack SizePriceAvailabilityQuantity
5 mg$48In Stock
10 mg$71In Stock
25 mg$148In Stock
50 mg$268In Stock
100 mg$397In Stock
200 mg$582In Stock
500 mg$913In Stock
1 mL x 10 mM (in DMSO)$50In Stock
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Purity:99.76%
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Product Introduction

Bioactivity
Description
Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.
Targets&IC50
5-HT1A receptor:30 nM (Ki), D1 receptor:83 nM (Ki), D4 receptor:4-15 nM (Ki), D3 receptor:0.71 nM (Ki), 5-HT7 receptor:86 nM (Ki), D2 receptor:4-15 nM (Ki), D5 receptor:4-15 nM (Ki)
In vitro
The selectivity of Rotigotine for D3 (pKi 9.2) receptors is higher 10-fold than D2/D4/D5 (pKi 8.5-8.0) and 100-fold than D1 receptors (pKi 7.2). Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. In functional studies, Rotigotine behaves as a full agonist at all dopamine receptors but notably, the potency for stimulation of D1 receptors is similar to that for D2/D3 receptors (pEC50 respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP+ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.
In vivo
In primed rats, Rotigotine (0.035/0.1/0.35 mg/kg) dose-dependently induces contralateral turning behavior. In drug-naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.
Kinase Assay
Binding assays are performed in 96-well polypropylene tubes in a final volume of 2?mL for D1 and D4 membranes and 1?mL for D2, D3 and D5 membranes containing: 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). Following 120?min of incubation at 25°C, bound radioligand is determined by rapid vacuum filtration through A/C glass fibre filters presoaked in 0.1% polyethylenimine. The filters are washed four times with 2?mL ice-cold ishing buffer (Tris-HCl 50?mM, pH?7.4 at 4°C) and retained radioactivity is determined by liquid scintillation counting.
AliasSPM 962, Neupro, N-0923, N-0437
Chemical Properties
Molecular Weight315.47
FormulaC19H25NOS
Cas No.99755-59-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 75 mg/mL (237.74 mM), Sonication is recommended.
Ethanol: 59 mg/mL (187 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.1699 mL15.8494 mL31.6987 mL158.4937 mL
5 mM0.6340 mL3.1699 mL6.3397 mL31.6987 mL
10 mM0.3170 mL1.5849 mL3.1699 mL15.8494 mL
20 mM0.1585 mL0.7925 mL1.5849 mL7.9247 mL
50 mM0.0634 mL0.3170 mL0.6340 mL3.1699 mL
100 mM0.0317 mL0.1585 mL0.3170 mL1.5849 mL

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