RS 17053 hydrochloride

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Cat.No. 0985 - RS 17053 hydrochloride | C24H29N2O2Cl.HCl | CAS No. 169505-93-5
Description: α1A antagonist
Chemical Name: (N-[2-(2-Cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine) hydrochloride
Datasheet
Citations
Reviews
Literature (4)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 4.49 10
DMSO 22.47 50

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 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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References

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 α1A1C)-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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