Biological Activity
Selective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively). Brain penetrant.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data
| M. Wt | 511.49 |
| Formula | C28H30N4O.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1226917-67-4 |
| PubChem ID | 75358288 |
| InChI Key | HEZIOTGUXSPDAK-UHFFFAOYSA-N |
| Smiles | O=C(N[C@@H]3CC[C@@H](CCN4CC(C=CC(C#N)=C5)=C5CC4)CC3)C1=C2C(C=CC=C2)=NC=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.57 | 50 | |
| water | 2.56 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 511.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.78 mL | 19.55 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.91 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Reavill et al (2000) Pharmacological actions of a novel, high-affinity, and selective human dopamine D3 receptor antagonist, SB-277011-A. J.Pharmacol.Exp.Ther. 294 1154 PMID: 10945872
Stemp et al (2000) Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): a potent and selective dopamine D3 receptor antagonist with high oral bioavailability and J.Med.Chem. 43 1878 PMID: 10794704
Keywords: SB 277011A dihydrochloride, supplier, SB277011A, dihydrochloride, dopamine, dopaminergic, receptors, antagonists, selective, d3, D3, Receptors, D3, Receptors, Tocris Bioscience
