Biological Activity
Subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels). Inhibits noradrenalin-induced contractions in rabbit vascular and lower urinary tissues.
Technical Data
| M. Wt | 645.19 |
| Formula | C36H40N4O5.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 157066-77-8 |
| PubChem ID | 56972175 |
| InChI Key | MXELDPKESKXREN-UHFFFAOYSA-N |
| Smiles | CC1=C(C(OC)=O)C(C2=CC=C([N+]([O-])=O)C=C2)C(C(NCCCN3CCC(C4=CC=CC=C4)(C5=CC=CC=C5)CC3)=O)=C(C)N1.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 | 64.52 | 100 | |
| ethanol | 64.52 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 645.19. 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 | 1.55 mL | 7.75 mL | 15.5 mL |
| 5 mM | 0.31 mL | 1.55 mL | 3.1 mL |
| 10 mM | 0.15 mL | 0.77 mL | 1.55 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
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References
References are publications that support the products' biological activity.
Wetzel et al (1995) Discovery of α1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. J.Med.Chem. 38 1579 PMID: 7752182
Leonardi et al (1997) Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15-2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, Part I. J.Pharmacol.Exp.Ther. 281 1272 PMID: 9190863
Kava et al (1998) α1L-adrenceptor 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
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