| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The molecular targets include dopamine D3 (Ki 0.71 nM), D2 (Ki 4–15 nM), D4 (Ki 3.9 nM), and D1 (Ki 83 nM) receptors, where rotigotine acts as an agonist; it is also a partial agonist at 5-HT1A receptors and an antagonist at α2B-adrenergic receptors, and its dopamine agonist activity underlies its efficacy in Parkinson’s disease and restless legs syndrome.
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|---|---|
| ln Vitro |
In vitro, (Rac)-rotigotine-d7 HCl competes with [3H]spiperone or a selective D3 radioligand for dopamine D3 receptors with a Ki of 0.71 nM and for D2 receptors with a Ki of 4–15 nM, activates D2/D3-mediated [35S]GTPγS binding and β-arrestin recruitment, and partially activates 5-HT1A receptors; the deuterated form retains dopamine agonist activity while enabling LC-MS/MS quantification.
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| ln Vivo |
In vivo, (Rac)-rotigotine-d7 HCl produces contralateral rotation in 6-OHDA-lesioned rats, improves motor function in MPTP-treated mice and primates, and reduces periodic limb movements in rodent models of restless legs syndrome; it is continuously delivered via transdermal patch, and the labeled form is used to quantify plasma and brain concentrations and dopamine receptor occupancy.
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| Enzyme Assay |
Noncellular binding assays incubate membrane homogenates expressing recombinant human D3, D2, D4, or D1 receptors with selective radioligands and increasing concentrations of (Rac)-rotigotine-d7 HCl; Ki values are calculated from displacement curves, and functional [35S]GTPγS binding or β-arrestin recruitment assays quantify agonist efficacy and potency at each subtype.
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| Cell Assay |
Cellular assays use CHO or HEK293 cells expressing D2 or D3 receptors and measure (Rac)-rotigotine-d7 HCl–stimulated [35S]GTPγS binding or inhibition of forskolin-stimulated cAMP; β-arrestin recruitment is assessed by enzyme complementation, and 5-HT1A partial agonist activity is measured in parallel.
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| Animal Protocol |
Animal protocols administer (Rac)-rotigotine-d7 HCl subcutaneously, intraperitoneally, or via transdermal patch to rats or mice at doses of 0.1–10 mg/kg; contralateral rotation in 6-OHDA-lesioned rats, motor function in MPTP-treated mice, and plasma and brain concentrations are measured by LC-MS/MS to relate dopamine receptor occupancy to behavioral efficacy.
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| References |
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| Molecular Formula |
C19H19D7CLNOS
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|---|---|
| Molecular Weight |
358.98
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
OC1=C2CCC(N(C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])CCC3=CC=CS3)CC2=CC=C1.Cl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7857 mL | 13.9284 mL | 27.8567 mL | |
| 5 mM | 0.5571 mL | 2.7857 mL | 5.5713 mL | |
| 10 mM | 0.2786 mL | 1.3928 mL | 2.7857 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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