Rotigotine

Agonist of dopamine D2/D3 receptor CAS# 99755-59-6

Rotigotine

2D Structure

Catalog No. BCC1907----Order now to get a substantial discount!

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Rotigotine

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Chemical Properties of Rotigotine

Cas No. 99755-59-6 SDF Download SDF
PubChem ID 57537 Appearance Powder
Formula C19H25NOS M.Wt 315.47
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 50 mg/mL (158.49 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol
SMILES CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
Standard InChIKey KFQYTPMOWPVWEJ-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H25NOS/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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Rotigotine Dilution Calculator

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Preparing Stock Solutions of Rotigotine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1699 mL 15.8494 mL 31.6987 mL 63.3975 mL 79.2468 mL
5 mM 0.634 mL 3.1699 mL 6.3397 mL 12.6795 mL 15.8494 mL
10 mM 0.317 mL 1.5849 mL 3.1699 mL 6.3397 mL 7.9247 mL
50 mM 0.0634 mL 0.317 mL 0.634 mL 1.2679 mL 1.5849 mL
100 mM 0.0317 mL 0.1585 mL 0.317 mL 0.634 mL 0.7925 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

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University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
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The University of Michigan
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Jilin University
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Wuhan University
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Universite de Paris
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Auckland University
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The University of Tokyo
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Korea University
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Background on Rotigotine

Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.

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References on Rotigotine

Pharmacokinetics of rotigotine transdermal system in adolescents with idiopathic restless legs syndrome (Willis-Ekbom disease).[Pubmed:28366342]

Sleep Med. 2017 Apr;32:48-55.

OBJECTIVE: To investigate the pharmacokinetics (PK) of Rotigotine transdermal system in adolescents with moderate-to-severe idiopathic restless legs syndrome (RLS). METHODS: This multicenter, open-label, dose-escalation study enrolled patients >/=13 to <18 years of age. Rotigotine transdermal patches were applied daily and up-titrated weekly: 0.5, 1, 2, 3 mg/24 h. Blood samples were collected on the final day of each dose step. Primary PK variables were the apparent total body clearance (CL/f; L/h) and volume of distribution at steady state (VSS/f; L) of unconjugated Rotigotine for each dose step, calculated for the PK per-protocol set (PKPPS). Other PK, safety, and efficacy variables (International RLS Study Group Rating Scale [IRLS]; Clinical Global Impressions Item 1 [CGI-1]) were assessed. RESULTS: Of 24 patients who received Rotigotine, 23 completed all dose steps and 17 formed the PKPPS. Least-squares mean (95% confidence interval) CL/f and VSS/f values were broadly similar across all dose steps (CL/f: 0.5 mg/24 h: 676.86 [408.50-1121.51]; 1 mg/24 h: 671.72 [459.11-982.80]; 2 mg/24 h: 937.56 [658.50-1334.89]; 3 mg/24 h: 1088.77 [723.47-1638.53]; VSS/f: 5403.16 [2850.67-10,241.17]; 6220.79 [3842.05-10,072.28]; 7114.01 [4547.88-11,128.07]; 6037.92 [3598.36-10,131.41]). Among 23 patients with efficacy data, mean IRLS and CGI-1 scores improved at each dosage level. Adverse events reported by >/=3 patients were nausea (seven) and application site reactions (four). CONCLUSIONS: Key PK properties of Rotigotine in adolescent patients with moderate-to-severe idiopathic RLS were comparable to those previously observed in adults. Rotigotine improved RLS symptoms and was well tolerated. ClinicalTrials.gov: NCT01495793.

Rotigotine may control drooling in patients with Parkinson's Disease: Preliminary findings.[Pubmed:28342306]

Clin Neurol Neurosurg. 2017 May;156:63-65.

OBJECTIVE: To evaluate the efficacy of Rotigotine in controlling the drooling of Parkinson's Disease (PD) patients. PATIENTS AND METHODS: We assessed 7 PD patients (Hoehn and Yahr scale >2.5) with three different clinical scores (Drooling Severity and Frequency Scale - DSFS, Drooling Rating Scale - DRS and Sialorrhea Clinical Scale for PD - SCS) before and after 4 weeks of therapy. Statistical differences were analyzed with Wilcoxon signed-rank test. RESULTS: We observed that Rotigotine significantly improves drooling as measured by the lowering of the three scores (p<0.05). CONCLUSIONS: Among non-motor symptoms of PD, drooling is one of the most embarrassing and disabling for patients. Current treatments are unsatisfactory and novel approaches are thus desirable. In this open-label pilot study we demonstrated on a small sample of patients that up to 4mg/24h of Rotigotine, a non-ergolinic dopamine agonist with continuous transdermal delivery, may be helpful in the management of drooling in advanced PD.

Levodopa, placebo and rotigotine change biomarker levels for oxidative stress.[Pubmed:28222651]

Neurol Res. 2017 May;39(5):381-386.

INTRODUCTION: Homocysteine increase and glutathione derivative cysteinyl-glycine fall are indirect biomarkers for oxidative stress, for instance due to dopamine D1 receptor stimulation. OBJECTIVES: To investigate the influence of the D1 receptor agonists levodopa and Rotigotine compared with placebo on homocysteine and cysteinyl-glycine in plasma of patients with Parkinson's disease. METHODS: Patients received 100 mg levodopa, 4 mg Rotigotine or placebo. Cysteinyl-glycine and homocysteine were measured every 30 min over three hours. RESULTS: Homocysteine rose during levodopa- and placebo administration. Rotigotine had no effect. Cysteine-glycine only increased after placebo- but not after levodopa- or Rotigotine. DISCUSSION: Homocysteine elevation results from hepatic and gastrointestinal methylation processes. Transdermal Rotigotine circumvents these methylation locations. Turnover of segregated alkyl residuals from Rotigotine serves as methyl group donors, which counteract homocysteine increment. The placebo-related cysteinyl-glycine increase results from reduced free radical exposure. Low levodopa dosing and antioxidants in the Rotigotine patch matrix prevented cysteinyl-glycine fall.

Description

Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

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