Biological Activity
Very selective β2 adrenergic antagonist/inverse agonist (Ki values are 1.2, 120 and 257 nM for β2, β1 and β3 receptors respectively). Active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Technical Data
| M. Wt | 313.87 |
| Formula | C17H27NO2.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 72795-01-8 |
| PubChem ID | 46704341 |
| InChI Key | KBXMBGWSOLBOQM-MELYUZJYSA-N |
| Smiles | CC1=C(CCC2)C2=C(OC[C@@H](O)[C@H](C)NC(C)C)C=C1.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 | 3.14 | 10 | |
| water | 3.14 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 313.87. 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 | 3.19 mL | 15.93 mL | 31.86 mL |
| 5 mM | 0.64 mL | 3.19 mL | 6.37 mL |
| 10 mM | 0.32 mL | 1.59 mL | 3.19 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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References
References are publications that support the products' biological activity.
Bilski et al (1983) The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551). J.Cardiovasc.Pharmacol. 5 430 PMID: 6191142
Cook et al (1993) β-Adrenoceptor subtypes and the opening of plasmalemmal K+-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue. Br.J.Pharmacol. 109 1140 PMID: 8104643
Strosberg and Pietri-Rouxel (1996) Function and regulation of the β3-adrenoceptor. TiPS 17 373 PMID: 8979772
Ten Berge et al (1995) β2-but not β3-adrenoceptors mediate prejunctional inhibition of non-adrenergic non cholinergic contraction of guinea pig main bronchi. Eur.J.Pharmacol. 275 199 PMID: 7796855
Bond et al (1995) Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor. Nature 374 272 PMID: 7885448
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