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(Rac)-Rotigotine

رقم الكتالوجGC71283

(Rac)-Rotigotine N-0437 هو راسيمات من روتيجوتين.

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(Rac)-Rotigotine التركيب الكيميائي

Cas No.: 92206-54-7

الحجم السعر المخزون الكميّة
5 mg
36٫00
متوفر
10 mg
58٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (Rac)-Rotigotine

(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine 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.

Rotigotine has a 10-fold selectivity for D3 (pKi=9.2) receptors compared with D2, D4 and D5 (pKi=8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pKi=7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC50 respectively: 9.0, 9.4-8.6, 9.7)[1].
Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. 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[4].
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References:
[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.
[2]. 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.
[3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91.
[4]. 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.

Chemical Properties of (Rac)-Rotigotine

Cas No. 92206-54-7 SDF
Formula C19H25NOS M.Wt 315.47
الذوبان Storage 4°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (Rac)-Rotigotine

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.1699 mL 15.8494 mL 31.6987 mL
5 mM 0.634 mL 3.1699 mL 6.3397 mL
10 mM 0.317 mL 1.5849 mL 3.1699 mL
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Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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