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Fosaprepitant dimeglumine salt

For research use only.

Catalog No.S3038 Synonyms: MK-0517

Fosaprepitant dimeglumine salt Chemical Structure

CAS No. 265121-04-8

Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

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10mM (1mL in DMSO) USD 590 In stock
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Biological Activity

Description Fosaprepitant dimeglumine salt (MK-0517) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
Targets
NK-1 receptor [1]
In vitro

Fosaprepitant (MK-0517, L-758,298) is a phosphoryl prodrug for aprepitant. Aprepitant is a selective substance P (NK-1 receptor) antagonist approved as part of combination therapy with a corticosteroid and a 5-HT 3 receptor antagonist for the prevention of acute and delayed Chemotherapy-induced nausea and vomiting. [1]

In vivo Fosaprepitant is converted to aprepitant within 30 min after intravenous administration via the action of ubiquitous phosphatases when administered intravenously. Fosaprepitant is well tolerated up to 150 mg (1 mg/ml), and Fosaprepitant 115 mg is bioequivalent in its AUC to aprepitant 125 mg. Fosaprepitant 115 mg has been submitted for FDA approval as an alternative on day 1 of a 3-day oral aprepitant regimen, with oral aprepitant administered on days 2 and 3. [1]

Protocol

Solubility (25°C)

In vitro DMSO 201 mg/mL (200.03 mM)
Water 135 mg/mL (134.35 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1004.83
Formula

C23H22F7N4O6P.2C7H17NO5

CAS No. 265121-04-8
Storage powder
in solvent
Synonyms MK-0517
Smiles CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NN(C(=O)N3)P(=O)(O)O)C4=CC=C(C=C4)F.CNCC(C(C(C(CO)O)O)O)O.CNCC(C(C(C(CO)O)O)O)O

In vivo Formulation Calculator (Clear solution)

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02407600 Unknown status Drug: FOSAPREPITANT (Emend)|Drug: Placebo Non-small Cell Lung Cancer|Vomiting|Nausea|Emesis Ajeet Gajra|Merck Sharp & Dohme Corp.|State University of New York - Upstate Medical University April 2015 Phase 2
NCT01074697 Completed Drug: Fosaprepitant dimeglumine|Drug: Placebo Nausea|Vomiting|Genital Neoplasms Female Odense University Hospital|Helsinn Healthcare SA April 2010 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID