Home Neuronal Signaling Neurokinin Receptor antagonist Fosaprepitant dimeglumine salt For research use only.

Fosaprepitant dimeglumine salt

Synonyms: MK-0517

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

Fosaprepitant dimeglumine salt Chemical Structure

Fosaprepitant dimeglumine salt Chemical Structure

CAS: 265121-04-8

Purity & Quality Control

Batch: Purity: 99.17%
99.17

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05755659 Recruiting Neoplasms Xijing Hospital July 15 2022 Not Applicable
NCT02407600 Unknown status Non-small Cell Lung Cancer|Vomiting|Nausea|Emesis Ajeet Gajra|Merck Sharp & Dohme LLC|State University of New York - Upstate Medical University April 2015 Phase 2
NCT01074697 Completed Nausea|Vomiting|Genital Neoplasms Female Odense University Hospital|Helsinn Healthcare SA April 2010 Phase 3

Chemical lnformation & Solubility

Molecular Weight 1004.83 Formula

C23H22F7N4O6P.2C7H17NO5
CAS No. 265121-04-8 SDF Download Fosaprepitant dimeglumine salt SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (99.51 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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