Biological Activity
Subtype-selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). Displays 126- and 50-fold selectivity over human α1B and α1D receptors respectively. Active in vivo.
Licensing Information
Sold with the permission of Roche Bioscience
Technical Data
| M. Wt | 462.89 |
| Formula | C20H25F3N4O3.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1215654-26-4 |
| PubChem ID | 11340200 |
| InChI Key | CWVABCXVOAVUJL-UHFFFAOYSA-N |
| Smiles | Cl.CC1=CNC(=O)N(CCCN2CCN(CC2)C2=C(OCC(F)(F)F)C=CC=C2)C1=O |
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
| Solubility | Soluble to 100 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 462.89. 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 | 2.16 mL | 10.8 mL | 21.6 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.32 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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References
References are publications that support the products' biological activity.
Conley et al (2001) The role of α1-adrenoceptors and 5-HT1A receptors in the control of the micturition reflex in male anaesthetized rats. Br.J.Pharmacol. 133 61 PMID: 11325795
Shannon Kava et al (1998) α1L-Adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man. Br.J.Pharmacol. 123 1359 PMID: 9579731
Williams et al (1999) In vitro α1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel α1A-adrenoceptor selective antagonists. Br.J.Pharmacol. 127 252 PMID: 10369480
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