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Fosaprepitant Dimeglumine | CAS 265121-04-8 | NK1 Receptor Antagonist Prodrug for Neurokinin Pathway Research
Original price was: $3.00.$2.00Current price is: $2.00.
Fosaprepitant Dimeglumine (CAS 265121-04-8) is a high-purity lyophilized powder supplied for preclinical research. It serves as a phosphorylated prodrug of aprepitant, used to investigate NK1 receptor signaling, neurokinin-1 pathway modulation, cytokine regulation, and cellular stress responses in molecular, cellular, and pharmacological studies.
Description
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. Its prodrug design enhances solubility and experimental handling while preserving pharmacological activity. Key applications include:
NK1 receptor pathway blockade and desensitization studies
Cytokine secretion and immune modulation assays
Neuroinflammatory model studies in vitro and in vivo
Ligand-receptor binding kinetics and pharmacodynamic studies
Oxidative stress and signaling pathway modulation
Preclinical pharmacokinetic and pharmacodynamic evaluations
The lyophilized powder format allows reconstitution in water or appropriate laboratory-grade buffers, enabling concentrations typically ranging from 1 to 50 mg/mL. Fosaprepitant Dimeglumine facilitates controlled and reproducible experimental conditions, providing a reliable platform for high-quality preclinical research.
Fosaprepitant Dimeglumine is also extensively used in combination studies to explore synergistic or antagonistic effects with other signaling modulators, kinase inhibitors, or neuroactive compounds. Its reproducibility and stability in lyophilized form make it a preferred choice for laboratories conducting comprehensive NK1 receptor research.
Product Specifications
| Parameter | Specification / Data |
|---|---|
| Chemical Name / Synonyms | Fosaprepitant Dimeglumine; Fosaprepitant Meglumine; Prodrug of Aprepitant; C23H22F7N4O6P·2(C7H17NO5) |
| CAS Number | 265121-04-8 |
| Molecular Formula | C23H22F7N4O6P·2(C7H17NO5) |
| Molecular Weight | 1004.0 g/mol |
| Purity / Assay | ≥99% |
| Appearance | White to off-white lyophilized powder |
| Dosage Form | Lyophilized powder for research use |
| Solubility | Water, DMSO, selected aqueous buffers |
| Concentration | Reconstitutable to 1–50 mg/mL depending on assay |
| Storage Temperature | 2–8 °C, protect from moisture and light |
| Stability | Highly stable lyophilized; avoid repeated freeze–thaw cycles |
| Analytical Methods | HPLC, MS, NMR verified; batch consistency confirmed |
| Mechanistic Target | NK1 receptor antagonist (via conversion to aprepitant) |
| Structural Category | NK1 receptor antagonist prodrug; phosphorylated small molecule |
| Applications | NK1 receptor studies, cytokine modulation, neuroimmune signaling, GPCR biology, receptor-ligand kinetics, in vivo pharmacology |
| Batch Consistency | Verified by HPLC, MS, NMR analyses |
| Regulatory Notes | For laboratory research use only |
| Origin | Factory small-molecule supplier; China chemical manufacturer; OEM & bulk production available |
| Additional Data | CoA provided for each batch |
Mechanism of Action
Prodrug Activation
Fosaprepitant Dimeglumine is enzymatically converted to aprepitant in plasma and tissues. This prodrug activation is predictable, ensuring consistent NK1 receptor antagonism for experimental studies. Fosaprepitant Dimeglumine’s conversion enhances solubility and facilitates handling in both in vitro and in vivo assays.
NK1 Receptor Antagonism
Upon conversion to aprepitant, Fosaprepitant Dimeglumine competitively inhibits Substance P binding, resulting in:
Inhibition of Gq/Gs-mediated signaling
Suppression of PLC/IP3-mediated calcium flux
Modulation of MAPK/ERK, JNK, and p38 pathways
Altered transcription factor activity (NF-κB, STAT, CREB)
Neuroimmune and Cytokine Modulation
Fosaprepitant Dimeglumine reduces NK1 receptor-mediated cytokine release, including IL-1β, IL-6, and TNF-α, affecting microglial and astrocyte activation and neurogenic inflammatory processes. Its use allows researchers to probe the influence of NK1 receptor antagonism on oxidative stress and neuroimmune signaling.
GPCR Signal Modulation
Fosaprepitant Dimeglumine and its active metabolite aprepitant influence:
β-arrestin recruitment and receptor internalization
cAMP/PKA signaling cascades
Regulation of stress-responsive transcriptional programs
Preclinical Research Applications
Fosaprepitant Dimeglumine is used for:
NK1 receptor desensitization studies
Ligand-receptor binding and kinetics assays
Cytokine profiling and neuroimmune modulation
Oxidative stress and intracellular signaling studies
Pharmacokinetic and pharmacodynamic modeling in preclinical animal studies
Fosaprepitant Dimeglumine’s lyophilized form ensures batch-to-batch reproducibility, stability, and accurate dosing for complex preclinical studies.
Side Effects (Preclinical Observations)
Cellular Effects
Reduced Substance P-mediated calcium flux
Modulated cytokine secretion patterns
Suppression of neurogenic inflammatory pathways
Biochemical Effects
Altered MAPK/ERK, JNK, and p38 signaling
Regulation of transcription factor activity (NF-κB, STAT, CREB)
Effects on oxidative stress signaling and apoptosis pathways
Handling Considerations
Use appropriate PPE and work in a fume hood
Store lyophilized Fosaprepitant Dimeglumine at 2–8 °C, protect from light and moisture
Strictly for laboratory research; not for human or veterinary use
Keywords
Fosaprepitant Dimeglumine, NK1 receptor antagonist, Substance P inhibitor, prodrug of aprepitant, neurokinin signaling research, cytokine modulation, GPCR biology, receptor-ligand kinetics, high-purity research chemical, factory small-molecule supplier, China chemical manufacturer, OEM & bulk production, laboratory research reagent
Shipping Guarantee
All shipments of Fosaprepitant Dimeglumine powder are handled using validated cold-chain logistics. Lyophilized powder is protected with moisture-proof and insulated packaging, shipped via express international couriers with full tracking and insurance.
Trade Assurance
Product authenticity is guaranteed. ≥99% purity verified by HPLC, MS, and NMR. CoA provided for every batch. Refund or replacement is available for any deviation from specifications.
Payment Support
Global payment options include PayPal, Visa, MasterCard, American Express, T/T, USDT, Bitcoin, and Ethereum. All transactions are encrypted and verified.
Disclaimer
Fosaprepitant Dimeglumine is for laboratory research only. Not for human or veterinary use. Researchers must adhere to institutional safety protocols.
References
Additional information
| Weight | 1.1 kg |
|---|---|
| Dimensions | 18 × 16 × 18 cm |
What is Fosaprepitant Dimeglumine used for in laboratory research?
Fosaprepitant Dimeglumine is a high-purity NK1 receptor antagonist prodrug used to study neurokinin signaling, cytokine modulation, GPCR pathways, and receptor-mediated intracellular signaling in preclinical molecular and cellular assays.
How is Fosaprepitant Dimeglumine converted to aprepitant?
Fosaprepitant Dimeglumine is enzymatically dephosphorylated in plasma and tissues to release aprepitant, which competitively inhibits Substance P binding to NK1 receptors, enabling precise pharmacological studies.
What is the purity of Fosaprepitant Dimeglumine supplied?
All batches of Fosaprepitant Dimeglumine are verified ≥99% purity by HPLC, MS, and NMR analyses to ensure consistency and reproducibility in preclinical research.
How should Fosaprepitant Dimeglumine lyophilized powder be stored?
Store at 2–8 °C, protected from light and moisture. Avoid repeated freeze-thaw cycles after reconstitution to maintain chemical stability.
Which solvents are suitable for reconstituting Fosaprepitant Dimeglumine?
Fosaprepitant Dimeglumine is soluble in water, DMSO, and selected laboratory-grade aqueous buffers, allowing flexible preparation for in vitro or in vivo assays.
Can Fosaprepitant Dimeglumine be used for GPCR signaling studies?
Yes, Fosaprepitant Dimeglumine (via aprepitant) blocks NK1 receptor GPCR signaling, regulating intracellular calcium, MAPK/ERK, JNK, and p38 pathways for mechanistic studies.
Is Fosaprepitant Dimeglumine suitable for cytokine modulation research?
Yes, preclinical studies show Fosaprepitant Dimeglumine inhibits NK1 receptor-mediated cytokine release, including IL-1β, IL-6, and TNF-α, useful for neuroimmune and inflammatory assays.
Can Fosaprepitant Dimeglumine be used in neuroinflammation models?
Yes, Fosaprepitant Dimeglumine is widely applied in vitro and in vivo to investigate NK1 receptor blockade effects on neuroinflammation, oxidative stress, and neuronal signaling.
Is bulk or OEM production of Fosaprepitant Dimeglumine available?
Yes, Fosaprepitant Dimeglumine is supplied by verified chemical manufacturers with OEM and bulk production options for preclinical laboratories.
What safety precautions are required when handling Fosaprepitant Dimeglumine?
Use appropriate PPE, including gloves and lab coats, work in a fume hood, and follow institutional safety protocols. The compound is strictly for research use only.
Can Fosaprepitant Dimeglumine be used in receptor-ligand binding assays?
Yes, Fosaprepitant Dimeglumine is ideal for NK1 receptor binding kinetics and ligand competition studies after conversion to aprepitant.
Which analytical methods confirm Fosaprepitant Dimeglumine quality?
Quality is confirmed using HPLC, MS, and NMR, with each batch supplied with a Certificate of Analysis (CoA) for verification.
Can Fosaprepitant Dimeglumine be used in in vivo preclinical models?
Yes, Fosaprepitant Dimeglumine’s water-soluble lyophilized form allows accurate dosing in animal models to study NK1 receptor antagonism, cytokine modulation, and neurokinin signaling.
Are high-purity Fosaprepitant Dimeglumine powders available?
Yes, all batches meet ≥99% purity standards, ensuring reliable results in preclinical pharmacological studies.
What research applications are suitable for Fosaprepitant Dimeglumine?
Fosaprepitant Dimeglumine is suitable for NK1 receptor studies, GPCR signaling, neuroimmune modulation, cytokine profiling, oxidative stress assays, receptor-ligand kinetics, and preclinical pharmacokinetic/pharmacodynamic investigations.
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