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Fosaprepitant dimeglumine

Fosaprepitant dimeglumine
Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.
Catalog No. T1790Cas No. 265121-04-8
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Fosaprepitant dimeglumine

Catalog No. T1790Cas No. 265121-04-8

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.
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Pack SizePriceAvailabilityQuantity
5 mg$45In Stock
10 mg$61In Stock
25 mg$123In Stock
50 mg$223In Stock
100 mg$369In Stock
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Product Introduction

Bioactivity
Description
Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.
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]
Kinase Assay
Biochemical Methods: EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
AliasL785298, MK-0517, Fosaprepitant dimeglumine salt
Chemical Properties
Molecular Weight1004.83
FormulaC37H56F7N6O16P
Cas No.265121-04-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 185 mg/mL (184.1 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 124 mg/mL (123.4 mM)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM0.9952 mL4.9760 mL9.9519 mL49.7597 mL
5 mM0.1990 mL0.9952 mL1.9904 mL9.9519 mL
10 mM0.0995 mL0.4976 mL0.9952 mL4.9760 mL
20 mM0.0498 mL0.2488 mL0.4976 mL2.4880 mL
50 mM0.0199 mL0.0995 mL0.1990 mL0.9952 mL
100 mM0.0100 mL0.0498 mL0.0995 mL0.4976 mL

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