169506-22-3
Chemical Structure
RS 17053 free base
- CAS No.: 169506-22-3
- Formula:C24H29ClN2O2
- Molecular Weight:412.96
IUPAC Name: 1-(5-chloro-1H-indol-3-yl)-N-(2-(2-(cyclopropylmethoxy)phenoxy)ethyl)-2-methylpropan-2-amine
InChIKey: XLZHXAXXJVKTFM-UHFFFAOYSA-N
SMILES: ClC=1C=CC=2NC=C(C2C1)CC(NCCOC=3C=CC=CC3OCC4CC4)(C)C
Biological Activity: RS 17053 free base is a selective α1A-adrenoceptor antagonist. RS 17053 free base binds to MrcA/MecA A-class penicillin-binding proteins, inhibits peptidoglycan biosynthesis, and binds to α1A and α1B/α1D-adrenoceptors. RS 17053 free base disrupts bacterial membranes, causing depolarization, ATP depletion, protein leakage, ROS accumulation, and upregulation of stress response genes. RS 17053 free base exerts bactericidal activity against Gram-positive/Gram-negative pathogens. RS 17053 free base can be used for research on bacterial infections and benign prostatic hyperplasia[1][2][3][4][5][6][7].
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RS 17053 free base | RS 17053 free base is a selective α1A-adrenoceptor antagonist. RS 17053 free base binds to MrcA/MecA A-class penicillin-binding proteins, inhibits peptidoglycan biosynthesis, and binds to α1A and α1B/α1D-adrenoceptors. RS 17053 free base disrupts bacterial membranes, causing depolarization, ATP depletion, protein leakage, ROS accumulation, and upregulation of stress response genes. RS 17053 free base exerts bactericidal activity against Gram-positive/Gram-negative pathogens. RS 17053 free base can be used for research on bacterial infections and benign prostatic hyperplasia. | |||||||||||||||||||||
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References
- [1]. Guo KX, et al. A novel penicillin-binding protein inhibitor with unprecedented intracellular activity eradicates multiple pathogenic bacteria. PLoS pathogens. 2026 Jul 16;22(7):e1014242.
- [2]. Muramatsu I, et al. Identification of α1L‐adrenoceptor in mice and its abolition by α1A‐adrenoceptor gene knockout. British journal of pharmacology. 2008 Dec;155(8):1224-34.
- [3]. Martin DJ. Preclinical pharmacology of α1-adrenoceptor antagonists. European urology. 1999 Jun 1;36(Suppl. 1):35-41.
- [4]. Baek S, et al. Repurposed membrane-targeting RS17053 eradicates MRSA persisters and enhances aminoglycoside killing. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2025 Dec;193:118763.
- [5]. Su TH, et al. Native profiles of α1A‐adrenoceptor phenotypes in rabbit prostate. British journal of pharmacology. 2008 Nov;155(6):906-12.
- [6]. Morishima S, et al. Identification of the alpha1L-adrenoceptor in rat cerebral cortex and possible relationship between alpha1L- and alpha1A-adrenoceptors. British journal of pharmacology. 2008 Apr;153(7):1485-94.
- [7]. Cleary L, et al. Sympathectomy reveals alpha 1A- and alpha 1D-adrenoceptor components to contractions to noradrenaline in rat vas deferens. British journal of pharmacology. 2004 Nov;143(6):745-52.