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Fosaprepitant Dimeglumine | CAS 265121-04-8 | NK1 Receptor Antagonist Prodrug for Neurokinin Pathway Research

Product Description

Fosaprepitant Dimeglumine (CAS 265121-04-8) is a phosphorylated prodrug of aprepitant extensively used in preclinical research to investigate NK1 receptor-mediated signaling, neurokinin pathways, and cytokine modulation. Fosaprepitant Dimeglumine’s lyophilized powder form provides enhanced solubility, precise dosing, and reproducibility in both in vitro and in vivo assays.

 

 

Pharmacological Background

The NK1 receptor is a G-protein-coupled receptor (GPCR) expressed in central and peripheral nervous systems, immune cells, and epithelial tissues. Its primary endogenous ligand, Substance P, mediates neurogenic inflammation, neurotransmission, and immune modulation. Fosaprepitant Dimeglumine, once enzymatically dephosphorylated, converts to aprepitant, a selective NK1 receptor antagonist, making it a reliable tool to study receptor desensitization, ligand binding kinetics, and downstream MAPK/ERK, JNK, and p38 signaling pathways.

Fosaprepitant Dimeglumine is widely used to explore:

 

 

Neuroimmune interactions and cytokine modulation (IL-1β, IL-6, TNF-α)

 

 

Central and peripheral nervous system stress responses

 

 

GPCR-mediated intracellular calcium signaling

 

 

MAPK/ERK, JNK, and p38 signal transduction

 

 

Receptor internalization and desensitization

 

 

Neuroinflammatory and oxidative stress models

 

 

Research Applications

Fosaprepitant Dimeglumine is applied in molecular, cellular, and pharmacological studies.

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Uploaded on November 14, 2025