Biological Activity
Selective NOP receptor antagonist (Ki values are 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively). Antagonizes the pronociceptive action of nociceptin (Cat. No. 0910) in an acute pain model. Potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
SB 612111 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 454.86 |
| Formula | C24H29Cl2NO.HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 371980-94-8 |
| PubChem ID | 21061234 |
| InChI Key | DCKUVQADDNMWEF-DQFHVVJASA-N |
| Smiles | CC1=CC=CC2=C1CC[C@H](CN3CCC(C4=C(Cl)C=CC=C4Cl)CC3)C[C@@H]2O.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 | 45.49 | 100 | |
| ethanol | 45.49 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 454.86. 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 | 2.2 mL | 10.99 mL | 21.98 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.4 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zaratin et al (2004) Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) J.Pharmacol.Exp.Ther. 308 454 PMID: 14593080
Rizzi et al (2007) Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vivo studies. J.Pharmacol.Exp.Ther. 321 968 PMID: 17329551
Spagnolo et al (2007) Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vitro studies. J.Pharm.Exp.Ther. 106 961 PMID:
Keywords: SB 612111 hydrochloride, supplier, SB612111, hydrochloride, opioids, NOP, receptors, antagonists, ORL1, N/OFQ, NOP, Receptors, NOP, Receptors, Tocris Bioscience
