| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
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| 50mg | |||
| Other Sizes |
| Targets |
D2 Receptor
Sumanirole targets the dopamine D2 receptor, acting as a selective agonist. It has Kis of 9.0 nM for D2, >7,140 nM for D1, 1,940 nM for D3, and >2,190 nM for D4 receptors, demonstrating high selectivity for D2. By activating the D2 receptor, sumanirole inhibits forskolin-stimulated cAMP accumulation. |
|---|---|
| ln Vitro |
Sumanirole is an extremely useful compound for fundamental research aimed at identifying neurobiological mechanisms based on a D2-linked (as opposed to D1, D3, D4, and D5-linked) dopamine mechanism of action.
Sumanirole is a dopamine D2 receptor agonist that is selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively). It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors with an EC50 of 17 nM. |
| ln Vivo |
Sumanirole has been studied in vivo for the treatment of Parkinson's disease and restless leg syndrome. However, it has never been approved for medical use. It is a valuable tool compound for basic research.
|
| Enzyme Assay |
Sumanirole is a dopamine receptor agonist, and its in vitro activity is assessed in radioligand binding and functional assays. In a typical binding assay, the compound is incubated with membranes expressing dopamine receptors and a radiolabeled ligand. The displacement of the radiolabeled ligand is measured, and the Ki is determined. In functional assays, the inhibition of forskolin-stimulated cAMP accumulation is measured.
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| Cell Assay |
Sumanirole is dissolved in DMSO and applied to cultured cells expressing dopamine receptors at concentrations ranging from 1 nM to 10 µM. The effect on cAMP accumulation is measured.
|
| ADME/Pharmacokinetics |
Sumanirole maleate has a molecular weight of 319.31 g/mol and a molecular formula of C15H17N3O5. It is a dopamine D2 receptor agonist. The compound is typically stored as a powder at -20°C for long-term stability. Sumanirole maleate is also known as U-95666E.
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| Toxicity/Toxicokinetics |
Sumanirole maleate has a manageable toxicity profile. Common side effects may include nausea, dizziness, and hypotension. No significant hepatotoxicity or nephrotoxicity has been reported.
|
| References | |
| Additional Infomation |
See also: Sumanirole (Note moved to).
Sumanirole maleate is a dopamine D2 receptor agonist that is selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively). It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors (EC50 = 17 nM). Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome. It is a valuable tool compound for basic research. |
| Molecular Formula |
C15H17N3O5
|
|---|---|
| Molecular Weight |
319.317
|
| Exact Mass |
319.116
|
| Elemental Analysis |
C, 56.42; H, 5.37; N, 13.16; O, 25.05
|
| CAS # |
179386-44-8
|
| Related CAS # |
179386-43-7; 179386-44-8
|
| PubChem CID |
9818478
|
| Appearance |
Solid powder
|
| LogP |
0.576
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
400
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C1NC2=C3N1C[C@H](NC)CC3=CC=C2.O=C(/C=C\C(O)=O)O
|
| InChi Key |
VOJRMYBBPKNLLI-ORHWHDKWSA-N
|
| InChi Code |
InChI=1S/C11H13N3O.C4H4O4/c1-12-8-5-7-3-2-4-9-10(7)14(6-8)11(15)13-9;5-3(6)1-2-4(7)8/h2-4,8,12H,5-6H2,1H3,(H,13,15);1-2H,(H,5,6)(H,7,8)/b;2-1-/t8-;/m1./s1
|
| Chemical Name |
(Z)-but-2-enedioic acid;(10R)-10-(methylamino)-1,3-diazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-2-one
|
| Synonyms |
PNU 95666; PNU-95666; U-95666E; U95666E; PNU95666; U 95666E; Sumanirole maleate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~156.6 mM)
H2O: ~10 mg/mL (~31.32 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (156.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1317 mL | 15.6583 mL | 31.3165 mL | |
| 5 mM | 0.6263 mL | 3.1317 mL | 6.2633 mL | |
| 10 mM | 0.3132 mL | 1.5658 mL | 3.1317 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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