[CAS NO. 265121-04-8] Fosaprepitant dimeglumine salt

Name: Fosaprepitant dimeglumine salt
Brand: Arctom Scientific
SKU: SLK-S3038

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PRODUCTS SPECIFICATIONS [265121-04-8]

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Catalog

SLK-S3038

Brand

Selleck

CAS

265121-04-8

DESCRIPTION [265121-04-8]

Overview

MDL	MFCD23102059
Molecular Weight	1004.83
Molecular Formula	C23H22F7N4O6P.2C7H17NO5
SMILES	[C@H]([C@@H]([C@@H](CO)O)O)([C@H](CNC)O)O.C(N1[C@]([C@@H](O[C@H](C)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)OCC1)(C3=CC=C(F)C=C3)[H])C4=NN(P(=O)(O)O)C(=O)N4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	0.9952 mL	4.9760 mL	9.9519 mL
5 mM	0.1990 mL	0.9952 mL	1.9904 mL
10 mM	0.0995 mL	0.4976 mL	0.9952 mL
50 mM	0.0199 mL	0.0995 mL	0.1990 mL

Description

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

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.

References

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

Synonyms

D-Glucitol, 1-deoxy-1-(methylamino)-, [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate (2:1)

D-Glucitol, 1-deoxy-1-(methylamino)-, [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate (2:1) (salt)

Phosphonic acid, [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]-, compd. with 1-deoxy-1-(methylamino)-D-glucitol (1:2)

Fosaprepitant dimeglumine

MK 0517

Fosaprepitant di(N-methylglucamine)