ICI 154129, a peptide analog, is a selective δ opioid antagonist.
CAT No: R1073
CAS No:83420-94-4
Synonyms/Alias:83420-94-4;ICI 154129;ICI 154,129;ICI-154129;UNII-97BUE7NR2M;(2S)-2-[[(2S)-2-[2-[[2-[[(2S)-2-[bis(prop-2-enyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]ethylsulfanyl]-3-phenylpropanoyl]amino]-4-methylpentanoic acid;N,N-Bis(allyl)-tyr-gly-gly-psi-methylthio-phe-leu;M 154,129;M-154,129;97BUE7NR2M;N,N-Bis(allyl)-tyrosyl-glycyl-glycyl-psi-methylthio-phenylalanyl-leucine;DTXSID00232349;N,N-Di-2-propenyl-L-tyrosylglycyl-(alphaS)-alpha-((2-aminoethyl)thio)benzenepropanoyl-L-leucine;Glycinamide, N,N-di-2-propenyl-L-tyrosyl-N-(2-((2-((1-carboxy-3-methylbutyl)amino)-2-oxo-1-(phenylmethyl)ethyl)thio)ethyl)-, (S-(R*,R*))-;L-Leucine, N,N-di-2-propenyl-L-tyrosylglycyl-(alphaS)-alpha-((2-aminoethyl)thio)benzenepropanoyl-;M-154129;L-LEUCINE, N,N-DI-2-PROPEN-1-YL-L-TYROSYLGLYCYL-(.ALPHA.S)-.ALPHA.-((2-AMINOETHYL)THIO)BENZENEPROPANOYL-;SCHEMBL4405821;ICI154129;ICI 154129;M 154129;M154129;M-154129;DTXCID50154840;AKOS024458661;HY-101233;CS-0021020;Q27272001;((S)-2-((2-(2-((S)-2-(Diallylamino)-3-(4-hydroxyphenyl)propanamido)acetamido)ethyl)thio)-3-phenylpropanoyl)-L-leucine;L-LEUCINE, N,N-DI-2-PROPEN-1-YL-L-TYROSYLGLYCYL-(ALPHAS)-ALPHA-((2-AMINOETHYL)THIO)BENZENEPROPANOYL-;
ICI 154,129 is a synthetic nonsteroidal compound recognized for its role as a selective estrogen receptor modulator (SERM). Structurally distinct from endogenous estrogens, it is designed to interact with estrogen receptors, particularly the estrogen receptor alpha (ERα), and modulate their activity in a tissue-dependent manner. Its unique pharmacological profile makes it a valuable molecular tool for probing estrogenic and antiestrogenic mechanisms in biochemical and molecular biology research. ICI 154,129 has been widely utilized in studies focused on dissecting estrogen receptor signaling, elucidating receptor-ligand interactions, and advancing the understanding of hormone-dependent physiological and pathological processes.
Receptor binding studies: As a potent SERM, ICI 154,129 is frequently employed in receptor binding assays to investigate the affinity, specificity, and kinetics of ligand interactions with estrogen receptors. Its well-characterized binding properties enable researchers to delineate the structural requirements for receptor activation or inhibition, supporting the development of new receptor modulators and enhancing the mechanistic understanding of ligand-receptor dynamics. By serving as a reference or competitor ligand, it provides critical insights into receptor occupancy, ligand displacement, and conformational changes associated with estrogen receptor engagement.
Signal transduction research: The compound is instrumental in exploring downstream signaling pathways initiated by estrogen receptor modulation. By selectively activating or inhibiting receptor subtypes in cell-based assays, ICI 154,129 facilitates the dissection of transcriptional and non-genomic signaling cascades. Researchers leverage its distinctive activity profile to map the effects of estrogenic modulation on gene expression, protein phosphorylation, and cellular responses, thereby contributing to the broader understanding of hormone-driven signaling networks in both normal and aberrant contexts.
Endocrine disruptor assessment: ICI 154,129 is utilized as a reference compound in evaluating the estrogenic or antiestrogenic potential of environmental chemicals and industrial compounds. Its defined activity on estrogen receptors makes it a benchmark for comparative studies, enabling toxicologists and environmental scientists to assess the impact of novel substances on endocrine signaling. Through in vitro and in vivo bioassays, ICI 154,129 aids in classifying compounds as endocrine disruptors and in establishing relevant dose-response relationships.
Hormone-dependent cancer research: The selective modulatory effects of ICI 154,129 on estrogen receptors render it a valuable tool in studies investigating the molecular basis of hormone-responsive cancers, such as breast and endometrial carcinomas. Researchers employ the compound to model estrogen receptor blockade or activation in cancer cell lines, elucidate resistance mechanisms to antiestrogen therapies, and characterize the interplay between receptor status and cellular proliferation. Its application in these experimental models supports the identification of new molecular targets and informs the rational design of next-generation SERMs.
Structure-activity relationship (SAR) studies: ICI 154,129 serves as a prototypical scaffold for SAR analyses aimed at optimizing nonsteroidal estrogen receptor modulators. By systematically modifying its chemical structure and evaluating the resulting analogs, medicinal chemists and pharmacologists gain valuable information about the molecular determinants of receptor selectivity, potency, and tissue specificity. These insights drive the rational design of novel compounds with improved pharmacological profiles, advancing the field of selective estrogen receptor modulation and supporting drug discovery efforts in hormone-related research.
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