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Fosaprepitant dimeglumine

Catalog No. T1790 CAS 265121-04-8

Synonyms: L785298, MK-0517, Fosaprepitant dimeglumine salt

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis.

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Fosaprepitant dimeglumine Chemical Structure

Fosaprepitant dimeglumine, CAS 265121-04-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 123.00
50 mg	In stock	$ 223.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

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Purity: 98.75%

Purity: 98%

Purity: 97.39%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents 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.

Synonyms	L785298, MK-0517, Fosaprepitant dimeglumine salt
Molecular Weight	1004.83
Formula	C37H56F7N6O16P
CAS No.	265121-04-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 185 mg/mL (184.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 124 mg/mL (123.4 mM)

References and Literature

1. Navari RM. Expert Opin Investig Drugs, 2007, 16(12), 1977-1985.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library FDA-Approved & Pharmacopeia Drug Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Keywords

Fosaprepitant dimeglumine 265121-04-8 GPCR/G Protein Neuroscience Neurokinin receptor nociception NK receptor MK0517 antagonist Aprepitant L785298 Inhibitor receptor chemotherapy-induced L-785298 nausea Tachykinin receptor MK-0517 substance-P inhibit Neurokinin Receptor vomiting neuropeptide L 785298 MK 0517 Fosaprepitant dimeglumine salt inhibitor

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