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Fosaprepitant

Product Name
Fosaprepitant
CAS No.
172673-20-0
Chemical Name
Fosaprepitant
Synonyms
L 758298;Fosaprepitant;Fosaprepitant D4;MK-0517 (Fosaprepitant);Fosaprepitant See F727305;Fosaprepitant (See also F727305);[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-2H-1,2,4-triazol-1-yl]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]phosphonic acid;P-[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]phosphonic Acid;Phosphonic acid, P-[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]-
CBNumber
CB11515191
Molecular Formula
C23H22F7N4O6P
Formula Weight
614.41
MOL File
172673-20-0.mol
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Fosaprepitant Property

Melting point:
>74°C (dec.)
Density 
1.65
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
DMSO, Methanol
pka
2.45±0.20(Predicted)
form 
Solid
color 
White
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ApexBio Technology
Product number
B1272
Product name
Fosaprepitant
Packaging
25mg
Price
$323
Updated
2021/12/16
ApexBio Technology
Product number
B1272
Product name
Fosaprepitant
Packaging
50mg
Price
$485
Updated
2021/12/16
Biorbyt Ltd
Product number
orb134399
Product name
Fosaprepitant
Purity
>99%
Packaging
100mg
Price
$510
Updated
2021/12/16
Biorbyt Ltd
Product number
orb134399
Product name
Fosaprepitant
Purity
>99%
Packaging
250mg
Price
$765
Updated
2021/12/16
Biorbyt Ltd
Product number
orb134399
Product name
Fosaprepitant
Purity
>99%
Packaging
1g
Price
$1504.5
Updated
2021/12/16
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Fosaprepitant Chemical Properties,Usage,Production

Chemical Properties

White Solid

Uses

Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

Uses

Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

Uses

An antiemetic drug, a Aprepitant prodrug.

Definition

ChEBI: A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triaz l-1-yl)phosphonic acid.

Biological Activity

fosaprepitant (l-758,298 mk-0517) is an antagonist of neurokinin-1[1].fosaprepitant has shown the pharmacodynamic function by its active metabolite aprepitant. fosaprepitanot has been found to be a highly selective antagonist of the nk-1 receptor and inhibit the cation of substance p. in addition, fosaprepitant has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. besides, because of the brain penetrating of aprepitant, fosaprepitant has been revealed to have a very high affinity for the nk-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. fosaprepitant has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (cinv) by combination with a 5-ht3 antagonist and a steroid [1].

Drug interactions

Potentially hazardous interactions with other drugs
Antidepressants: avoid with St John’s wort.
Antipsychotics: avoid with pimozide.
Cytotoxics: possibly increases bosutinib concentration - avoid or reduce bosutinib dose.
Oestrogens and progestogens: may cause contraceptive failure.

Metabolism

Fosaprepitant is a prodrug and is rapidly metabolised to aprepitant. Aprepitant undergoes extensive hepatic metabolism, mainly via oxidation by the cytochrome P450 isoenzyme CYP3A4; the isoenzymes CYP1A2 and CYP2C19 mediate minor metabolic pathways. The resultant metabolites have weak activity and are excreted in the urine and in the faeces.

References

[1] van belle sj1, cocquyt v. fosaprepitant dimeglumine (mk-0517 or l-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting.expert opin pharmacother. 2008 dec; 9(18):3261-70.

Fosaprepitant Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Fosaprepitant manufacturers

Hebei Mingeng Biotechnology Co., Ltd
Product
Fosaprepitant 172673-20-0
Price
US $200.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000kg/Month
Release date
2022-11-24
Shijiazhuang Gantuo Biotechnology Co., Ltd
Product
Fosaprepitant 172673-20-0
Price
US $100.00/KG
Min. Order
25KG
Purity
99%
Supply Ability
1000 Kilogram/Kilograms per Week
Release date
2023-03-10
Wuhan Monad Medicine Tech Co.,LTD
Product
Fosaprepitant 172673-20-0
Price
US $10.00/KG
Min. Order
1Kg/Bag
Purity
99%min
Supply Ability
20000
Release date
2020-12-22

172673-20-0, FosaprepitantRelated Search:


  • [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-2H-1,2,4-triazol-1-yl]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]phosphonic acid
  • L 758298
  • P-[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]phosphonic Acid
  • MK-0517 (Fosaprepitant)
  • 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)
  • Fosaprepitant
  • Fosaprepitant (See also F727305)
  • Phosphonic acid, P-[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]-
  • Fosaprepitant See F727305
  • Fosaprepitant D4
  • 172673-20-0
  • C23H22F7N4O6P
  • Aromatics
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Pharmaceuticals