1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    Adrenergic Receptor
    5-HT Receptor
  3. (Rac)-Rotigotine hydrochloride

(Rac)-Rotigotine hydrochloride 

Cat. No.: HY-15394 Purity: 97.76%
Handling Instructions

(Rac)-Rotigotine hydrochloride 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.

For research use only. We do not sell to patients.

(Rac)-Rotigotine hydrochloride Chemical Structure

(Rac)-Rotigotine hydrochloride Chemical Structure

CAS No. : 102120-99-0

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10 mM * 1  mL in DMSO USD 66 In-stock
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100 mg USD 216 In-stock
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Description

(Rac)-Rotigotine hydrochloride 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.

IC50 & Target[1][2]

D3 Receptor

0.71 nM (Ki)

D2 Receptor

13.5 nM (Ki)

D4 Receptor

3.9-15 nM (Ki)

D5 Receptor

5.4 nM (Ki)

D1 Receptor

83 nM (Ki)

5-HT1A Receptor

30 nM (Ki)

5-HT2B Receptor

27 nM (Ki)

In Vitro

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].
.

Molecular Weight

351.93

Formula

C₁₉H₂₆ClNOS

CAS No.

102120-99-0

SMILES

OC1=C2CCC(N(CCC)CCC3=CC=CS3)CC2=CC=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (142.07 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(Rac)-RotigotineDopamine ReceptorAdrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptoragonistactivatorInhibitorinhibitorinhibit

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Product Name:
(Rac)-Rotigotine hydrochloride
Cat. No.:
HY-15394
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