Biological Activity
Highly selective and potent β1-adrenoceptor antagonist (IC50 = 0.7 nM). Displays 10,000-fold selectivity over β2-adrenoceptors. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
Technical Data
| M. Wt | 567.39 |
| Formula | C23H25F3N4O5.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 1216905-73-5 |
| PubChem ID | 56972164 |
| InChI Key | PURFQCFKYNMIQF-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CN1C=C(N=C1C1=CC=C(OCC(O)CNCCOC2=CC=C(O)C(=C2)C(N)=O)C=C1)C(F)(F)F |
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 | 24.72 | 50 | |
| ethanol | 49.45 | 100 | |
| water | 24.72 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 567.39. 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 | 1.76 mL | 8.81 mL | 17.62 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Dooley et al (1986) CGP 20712A: a useful tool for quantitating β1- and β2-adrenoceptors. Eur.J.Pharmacol. 130 137 PMID: 2877892
Hieble et al (1995) α-and β-adrenoceptors. From the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J.Med.Chem. 38 3415 PMID: 7658428
Kitagawa et al (1995) Determination of β-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective β-antagonists. Br.J.Pharmacol. 116 1635 PMID: 8564230
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