GRADE & PURITY 10mM in DMSO

Synonyms

MK-0517 | 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)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonyms

MK-0517 | 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)

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Mechanism of action

Neurokinin 1 receptor antagonist

Names and Identifiers

• Isomeric SMILES: C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)CC3=NN(C(=O)N3)P(=O)(O)O)C4=CC=C(C=C4)F.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O
• Alternate CAS: 172673-20-0
• PubChem CID: 135564864
• Molecular Weight: 1004.83