Biological Activity
α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8).
Licensing Information
Sold with the permission of Roche Bioscience
Compound Libraries
RS 17053 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 449.42 |
| Formula | C24H29N2O2Cl.HCl |
| Storage | Store at RT |
| CAS Number | 169505-93-5 |
| PubChem ID | 9824953 |
| InChI Key | QFOPFGRPNPCPBX-UHFFFAOYSA-N |
| Smiles | Cl.CC(C)(CC1=CNC2=CC=C(Cl)C=C12)NCCOC1=C(OCC2CC2)C=CC=C1 |
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 | 22.47 | 50 | |
| ethanol | 4.49 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 449.42. 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 | 2.23 mL | 11.13 mL | 22.25 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Ford et al (1996) RS 17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine hydrochloride, a selective α1A-adrenoceptor antagonist, displays low affinity for functional α1-adrenoceptors in huma Mol.Pharmacol. 49 209 PMID: 8632751
Marshall et al (1996) Different subtypes of α1A-adrenoceptor mediating contraction of rat epididymal vas deferens, rat hepatic portal vein and human prostate distinguished by the antagonist RS 17053. Br.J.Pharmacol. 119 407 PMID: 8886428
Ford et al (1995) Do α1A (α1C)-adrenoceptors (AR) mediate prostatic smooth muscle contraction in man? Studies with a novel, selective α1A-AR antagonist, RS 17053. Br.J.Pharmacol. 114 C25 PMID:
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