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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
Molecular Weight:
614.41
MDL Number:
MFCD00942401
MOL File:
172673-20-0.mol
MSDS File:
SDS
Last updated:2023-05-18 11:30:59

Fosaprepitant Properties

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
FDA UNII 6L8OF9XRDC

Pharmacokinetic data

Protein binding 97%
Volume of distribution 82 Litres
Biological half-life 11 / Unchanged

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338

Fosaprepitant price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ApexBio Technology B1272 Fosaprepitant 172673-20-0 25mg $323 2021-12-16 Buy
ApexBio Technology B1272 Fosaprepitant 172673-20-0 50mg $485 2021-12-16 Buy
Biorbyt Ltd orb134399 Fosaprepitant >99% 172673-20-0 100mg $510 2021-12-16 Buy
Biorbyt Ltd orb134399 Fosaprepitant >99% 172673-20-0 250mg $765 2021-12-16 Buy
Biorbyt Ltd orb134399 Fosaprepitant >99% 172673-20-0 1g $1504.5 2021-12-16 Buy
Product number Packaging Price Buy
B1272 25mg $323 Buy
B1272 50mg $485 Buy
orb134399 100mg $510 Buy
orb134399 250mg $765 Buy
orb134399 1g $1504.5 Buy

Fosaprepitant Chemical Properties,Uses,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

An antiemetic drug, a Aprepitant prodrug.

Uses

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

Global( 124)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 - 03@ sales03@shyrchem.com CHINA 738 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Shanghai Yingrui Biopharma Co.,Ltd
21-33585366 export01@shyrchem.com CHINA 1320 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427 sales@conier.com China 47465 58
Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd
+86-86-22-87899925 +86-8618522618860 18522618860@163.com China 694 58
Wuhan Monad Medicine Tech Co.,LTD
02768782018 18771942761 sales01@whmonad.com CHINA 992 58
Shanxi Xuanran Import and Export Trade Co., Ltd.
+8617735180244 mike_yan@xuanranglobal.com CHINA 4022 58

View Lastest Price from Fosaprepitant manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Fosaprepitant pictures 2023-06-26 Fosaprepitant
172673-20-0
US $200.00 / kg 1kg 99% 1000kg/Month Hebei Mingeng Biotechnology Co., Ltd
Fosaprepitant pictures 2023-04-11 Fosaprepitant
172673-20-0
US $100.00 / KG 25KG 99% 1000 Kilogram/Kilograms per Week Shijiazhuang Gantuo Biotechnology Co., Ltd
Fosaprepitant pictures 2021-08-31 Fosaprepitant
172673-20-0
US $10.00 / KG 1Kg/Bag 99%min 20000 Wuhan Monad Medicine Tech Co.,LTD
  • Fosaprepitant pictures
  • Fosaprepitant
    172673-20-0
  • US $200.00 / kg
  • 99%
  • Hebei Mingeng Biotechnology Co., Ltd
  • Fosaprepitant pictures
  • Fosaprepitant
    172673-20-0
  • US $100.00 / KG
  • 99%
  • Shijiazhuang Gantuo Biotechnology Co., Ltd
  • Fosaprepitant pictures
  • Fosaprepitant
    172673-20-0
  • US $10.00 / KG
  • 99%min
  • Wuhan Monad Medicine Tech Co.,LTD

Fosaprepitant Spectrum

[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