Biological Activity
Potent and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). Orally active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
Compound Libraries
SR 59230A hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 361.91 |
| Formula | C21H27NO2.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1135278-41-9 |
| PubChem ID | 24978529 |
| InChI Key | SHUCXUIOEAAJJL-MKSBGGEFSA-N |
| Smiles | O[C@@H](CN[C@H]2CCCC3=C2C=CC=C3)COC1=C(CC)C=CC=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 | 36.19 | 100 | |
| water | 3.62 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 361.91. 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 | 2.76 mL | 13.82 mL | 27.63 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Manara et al (1996) Functional identification of rat atypical β-adrenoceptors by the first β3-selective antagonists, aryloxypropanolaminotetralins. Br.J.Pharmacol. 117 435 PMID: 8821531
Mizuno et al (2002) Stimulation of β3-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Br.J.Pharmacol. 135 951 PMID: 11861323
Manara et al (1995) Aryloxypropanolaminotetralins are the first selective antagonists for atypical (β3) β-adrenoceptors. Pharmacol.Comm. 6 253 PMID:
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