Biological Activity
Potent and selective α2 antagonist at pre- and post-junctional α2-adrenoceptors (Ki values are 13 and 17 nM respectively). Exhibits antihypertensive activity in a rat model.
Technical Data
| M. Wt | 232.15 |
| Formula | C11H14ClN.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 86129-54-6 |
| PubChem ID | 10220250 |
| InChI Key | JKQKVNMNAIFCFS-UHFFFAOYSA-N |
| Smiles | CN2CCC1=CC=CC(Cl)=C1CC2.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 | 23.21 | 100 | |
| water | 23.21 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 232.15. 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 | 4.31 mL | 21.54 mL | 43.08 mL |
| 5 mM | 0.86 mL | 4.31 mL | 8.62 mL |
| 10 mM | 0.43 mL | 2.15 mL | 4.31 mL |
| 50 mM | 0.09 mL | 0.43 mL | 0.86 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Roesler et al (1986) Characterization of the antihypertensive activity of SK&F 86466, a selective alpha-2 antagonist, in the rat. J.Pharmacol.Exp.Ther. 236 1 PMID: 2867209
Schafers et al (1990) An evaluation of the alpha-adrenoceptor antagonism produced by SK&F 86466 in healthy normotensive males. Br.J.Clin.Pharmacol. 30 884 PMID: 1981137
Hieble et al (1985) Selective Alpha-2 adrenoceptor blockade by SK&F 86466: in vitro characterization of receptor sensitivity. J.Pharmacol.Exp.Ther. 236 90 PMID:
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