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RS 17053 hydrochloride

Catalog No. T16798   CAS 169505-93-5
Synonyms: RS-17053

RS 17053 hydrochloride is a potent and selective antagonist of α1A adrenoceptor. RS 17053 hydrochloride exhibits a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

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RS 17053 hydrochloride Chemical Structure
RS 17053 hydrochloride, CAS 169505-93-5
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2 mg In stock $ 34.00
5 mg In stock $ 55.00
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1 mL * 10 mM (in DMSO) In stock $ 65.00
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Purity: 99.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RS 17053 hydrochloride is a potent and selective antagonist of α1A adrenoceptor. RS 17053 hydrochloride exhibits a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
Targets&IC50 α1A:(pki)9.1 , α1A:9.8(PA2)
In vitro RS 17053 hydrochloride antagonizes responses to NE only at high concentrations in isolated smooth muscle preparations from human LUT tissues. RS 17053 hydrochloride displays a high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8) in several tissues from rat and cloned adrenoceptors [1].
In vivo RS 17053 hydrochloride has a rapid onset of action and a duration of action exceeding 60 min. RS-17053 (10 mg/kg ) significantly suppresses food intake. RS 17053 hydrochloride pretreatment obviously alters food intake [F(4, 132) 5 6.28, p, 0.0001] [2].
Synonyms RS-17053
Molecular Weight 449.41
Formula C24H30Cl2N2O2
CAS No. 169505-93-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (278.14 mM)

TargetMolReferences and Literature

1. Ford AP, et al. RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha, alpha-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective alpha 1A-adrenoceptor antagonist, displays low affinity for functional alpha 1-adrenoceptors in human prostate: implications for adrenoceptor classification. Mol Pharmacol. 1996 Feb;49(2):209-15. 2. Wellman PJ, et al. Effects of the alpha 1a-adrenoceptor antagonist RS-17053 on phenylpropanolamine-induced anorexia in rats. Pharmacol Biochem Behav. 1997 May-Jun;57(1-2):281-4.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library

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Keywords

RS 17053 hydrochloride 169505-93-5 GPCR/G Protein Neuroscience Others Adrenergic Receptor Beta Receptor RS17053 inhibit RS17053 Hydrochloride RS 17053 Hydrochloride RS 17053 Inhibitor RS-17053 RS-17053 Hydrochloride inhibitor

 

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