CAS 265121-04-8

Fosaprepitant dimeglumine

Description:

Fosaprepitant dimeglumine is a synthetic compound primarily used as an antiemetic in the prevention of nausea and vomiting associated with chemotherapy. It is a prodrug of aprepitant, which acts as a selective antagonist of the neurokinin-1 (NK1) receptor, thereby inhibiting the action of substance P, a neuropeptide involved in the vomiting reflex. The substance is characterized by its high solubility in water due to the presence of the dimeglumine moiety, which enhances its bioavailability. Fosaprepitant is typically administered intravenously and is known for its efficacy in combination with other antiemetic agents. Its pharmacokinetics include rapid conversion to aprepitant in the body, with a relatively long half-life, allowing for sustained antiemetic effects. Common side effects may include fatigue, dizziness, and gastrointestinal disturbances. As a therapeutic agent, fosaprepitant dimeglumine plays a crucial role in improving the quality of life for patients undergoing cancer treatment by effectively managing chemotherapy-induced nausea and vomiting.

Formula: C₂₃H₂₂F₇N₄O₆P·2C₇H₁₇NO₅

InChI: InChI=1S/C23H22F7N4O6P.C7H17NO5/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)40-20-19(13-2-4-17(24)5-3-13)33(6-7-39-20)11-18-31-21(35)34(32-18)41(36,37)38;1-8-2-4(10)6(12)7(13)5(11)3-9/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38);4-13H,2-3H2,1H3/t12-,19+,20-;4-,5+,6+,7+/m10/s1

InChI key: InChIKey=UGJUJYSRBQWCEK-GGXTVIBHSA-N

SMILES: C(N1[C@H]([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)C4=NN(P(=O)(O)O)C(=O)N4.[C@H]([C@@H]([C@@H](CO)O)O)([C@H](CNC)O)O

Synonyms:

• 1-Deoxy-1-(Methylamino)-D-Glucitol [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
• <span class="text-smallcaps">D</span>-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)
• <span class="text-smallcaps">D</span>-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)
• 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)
• Fosaprepitant di(N-methylglucamine)
• Fosaprepitant dimeglumine [USAN]
• Ivemend
• Mk-0517
• 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)
• 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)-<span class="text-smallcaps">D</span>-glucitol (1:2)
• Unii-D35Fm8T64X
• Fosaprepitant dimeglumine
• Fosapitant Dimeglumine

Fosaprepitant dimeglumine

CAS: 265121-04-8

Formula: C₃₇H₅₆F₇N₆O₁₆P

Purity: 98%

Color and Shape: Solid

Molecular weight: 1004.8337

Ref: IN-DA00BF3G

Fosaprepitant dimeglumine

CAS: 265121-04-8

Fosaprepitant dimeglumine

Purity: ≥95%

Molecular weight: 1004.83g/mol

Ref: 54-BUP10189

Fosaprepitant Dimeglumine

CAS: 265121-04-8

Formula: C₂₃H₂₂F₇N₄O₆P·2C₇H₁₇NO₅

Color and Shape: White To Off-White Solid

Molecular weight: 614.41 2*195.22

Ref: 4Z-F-361

Fosaprepitant-d4 Dimeglumine

CAS: 265121-04-8

Formula: C₂₃H₁₈D₄F₇N₄O₆P·2C₇H₁₇NO₅

Color and Shape: White To Off-White Solid

Molecular weight: 618.44 2*195.22

Ref: 4Z-F-364

Fosaprepitant Dimeglumine

CAS: 265121-04-8

Formula: C₂₃H₂₂F₇N₄O₆P·2C₇H₁₇NO₅

Purity: >95.0%(HPLC)(qNMR)

Color and Shape: White to Light yellow powder to crystal

Molecular weight: 1,004.84

Ref: 3B-F1355

Fosaprepitant dimeglumine

CAS: 265121-04-8

Fosaprepitant dimeglumine (MK-0517) is a soluble prodrug of aprepitant, which prevents nausea by blocking NK1 receptors.

Formula: C₃₇H₅₆F₇N₆O₁₆P

Purity: 98% - 99.03%

Color and Shape: Solid

Molecular weight: 1004.83

Ref: TM-T1790

Fosaprepitant Impurity 10

CAS: 265121-04-8

Formula: C₂₃H₂₂F₇N₄O₇P

Color and Shape: White To Off-White Solid

Molecular weight: 630.42

Ref: 4Z-F-3617

Fosaprepitant-d4 Dimeglumine

Controlled Product

CAS: 265121-04-8

Applications Fosaprepitant-d4 Dimeglumine is a labeled analogue of Fosaprepitant Dimeglumine (F727305), a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.
References Tattersall, F., et al.: Neuropharmacol., 39, 652 (2000), Cocquyt, V., et al.: Eur. J. Canc., 37, 835 (2001), Lasseter, K., et al.: J. Clin. Pharmacol., 47, 834 (2007), Marbury, T., et al.: Anesthes., Analges., 109, 418 (2009),

Formula: C₃₇H₅₂D₄F₇N₆O₁₆P

Color and Shape: Neat

Molecular weight: 1008.86

Ref: TR-F727307

Bis((2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol); (3-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid

CAS: 265121-04-8

Purity: 98.05%

Molecular weight: 1004.844

Ref: 10-F979755

Fosaprepitant Dimeglumine

Controlled Product

CAS: 265121-04-8

Applications Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.
References Tattersall, F., et al.: Neuropharmacol., 39, 652 (2000), Cocquyt, V., et al.: Eur. J. Canc., 37, 835 (2001), Lasseter, K., et al.: J. Clin. Pharmacol., 47, 834 (2007), Marbury, T., et al.: Anesthes., Analges., 109, 418 (2009),

Formula: C₂₃H₂₂F₇N₄O₆P·2C₇H₁₇NO₅

Color and Shape: White To Off-White

Molecular weight: 1004.83

Ref: TR-F727305

1-Deoxy-1-(methylamino)-D-glucitol [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]m ethyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate

CAS: 265121-04-8

Fosaprepitant is a drug that belongs to the class of drugs used for chemotherapy. It is a prodrug that is converted in vivo to aprepitant, its active form. Fosaprepitant acts as an antagonist of the neurokinin-1 receptor (NK-1R) and inhibits the binding of substance P, which leads to an anti-inflammatory effect. Fosaprepitant has been shown to inhibit the production of substance P in animal models, leading to a reduction in inflammation. In clinical trials, fosaprepitant has been shown to be safe and well tolerated when used with other drugs such as cisplatin and docetaxel in patients with cancer.

Formula: C₂₃H₂₂F₇N₄O₆P•(C₇H₁₇NO₅)₂

Purity: Min. 95%

Color and Shape: White To Off-White Solid

Molecular weight: 1,004.83 g/mol

Ref: 3D-FD46503

Fosaprepitant-13C,15N3 Dimeglumine

Controlled Product

CAS: 265121-04-8

Formula: C₃₆CH₅₆F₇N₃N₃O₁₆P

Color and Shape: Neat

Molecular weight: 1008.82

Ref: TR-F727308