Ubrogepant, also known as MK-1602, is a potent and selective oral calcitonin gene-related peptide (CGRP) receptor antagonist.
CAT No: 10-101-185
CAS No:1374248-77-7
Synonyms/Alias:MK-1602; MK 1602; MK1602
Ubrogepant is a small-molecule calcitonin gene-related peptide (CGRP) receptor antagonist that has garnered significant attention within neuropharmacology and peptide receptor research. As a structurally defined, non-peptide compound, it exhibits high specificity for the human CGRP receptor, making it an invaluable tool for studies investigating the physiological and biochemical roles of CGRP signaling in the central and peripheral nervous systems. Its unique binding profile and receptor selectivity provide researchers with a reliable means of modulating CGRP-mediated pathways, thereby enabling detailed exploration of neuropeptide function, receptor pharmacodynamics, and related signaling cascades.
Neuropharmacology research: Ubrogepant serves as a critical molecular probe for dissecting the mechanisms of CGRP receptor activation and inhibition within neuronal tissues. By enabling selective antagonism of the CGRP receptor, it allows researchers to delineate the contributions of CGRP signaling to synaptic transmission, neuronal excitability, and neurogenic inflammation. Its application extends to in vitro and ex vivo systems, where it facilitates the study of receptor-ligand dynamics, downstream signaling events, and the modulation of neuropeptide release under controlled experimental conditions.
Receptor binding assays: The compound's high affinity and selectivity make it particularly suited for competitive binding studies aimed at characterizing CGRP receptor pharmacology. Utilizing radioligand or fluorescence-based assays, scientists can employ ubrogepant to quantify receptor occupancy, assess binding kinetics, and evaluate the effects of allosteric modulators or endogenous ligands. Such assays are essential for mapping receptor distribution, understanding receptor-ligand interactions at the molecular level, and validating the specificity of new CGRP-targeted compounds.
Signal transduction studies: Ubrogepant is widely used in cell-based assays to investigate the downstream effects of CGRP receptor inhibition on intracellular signaling pathways. Its ability to block CGRP-induced cAMP accumulation and other second messenger responses enables precise analysis of signal transduction networks. Researchers can thereby elucidate the role of CGRP in modulating cellular responses such as gene expression, protein phosphorylation, and ion channel activity, shedding light on the broader implications of CGRP signaling in neurobiology and vascular physiology.
Pharmacokinetic and metabolic profiling: The well-characterized chemical structure of ubrogepant makes it an excellent candidate for in vitro metabolic stability and pharmacokinetic studies. Researchers can utilize the compound to assess absorption, distribution, metabolism, and excretion (ADME) properties in various biological matrices, including liver microsomes and hepatocyte cultures. Such investigations are crucial for understanding the metabolic fate of CGRP antagonists, identifying potential metabolites, and optimizing compound design for improved bioavailability and stability in drug discovery settings.
Chemical synthesis and analytical method development: Ubrogepant's defined synthetic pathway and analytical detectability support its use as a reference standard or quality control material in synthetic chemistry and analytical laboratories. Its application in method validation, including liquid chromatography-mass spectrometry (LC-MS) and high-performance liquid chromatography (HPLC), allows for the accurate quantification and purity assessment of CGRP receptor antagonists and related analogs. This facilitates the development and optimization of robust analytical protocols necessary for compound characterization, stability testing, and batch-to-batch consistency evaluation in research and industrial environments.
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