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Submit ReviewRS 17053 hydrochloride
Description: α1A antagonist
Chemical Name: (N-[2-(2-Cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine) hydrochloride
Biological Activity for RS 17053 hydrochloride
RS 17053 hydrochloride is an 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
Technical Data for RS 17053 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RS 17053 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 4.49 | 10 | |
| DMSO | 22.47 | 50 |
Preparing Stock Solutions for RS 17053 hydrochloride
The following data is based on the product molecular weight 449.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.45 mL | 22.25 mL | 44.5 mL |
| 2.5 mM | 0.89 mL | 4.45 mL | 8.9 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.89 mL |
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Product Datasheets for RS 17053 hydrochloride
References for RS 17053 hydrochloride
References are publications that support the biological activity of the product.
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
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Literature in this Area
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.