Rotigotine- NEW
Price | $48 | $71 | $148 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: Rotigotine- | CAS No.: 99755-59-6 |
Purity: 99.76% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | Rotigotine- |
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. |
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. |
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. |
Storage | Powder: -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) |
Keywords | Rotigotine | dopamine | 5-HT1A | Adrenergic Receptor | receptor | N0437 | Serotonin Receptor | 5-HT Receptor | Beta Receptor | N 0437 | N0923 | 5-hydroxytryptamine Receptor | Dopamine Receptor | α2B-adrenergic | Inhibitor | SPM962 | Rotigotine- | inhibit | SPM-962 | N 0923 |
Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Octopamine hydrochloride | Oxolinic acid | Trazodone hydrochloride | Mianserin hydrochloride |
Related Compound Libraries | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | GPCR Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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