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
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 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | 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 |
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
Supplier | Tel | 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 +8613203830695 | sales@coreychem.com | China | 29888 | 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 | +86-023-6139-8061 +86-86-13650506873 | 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 | 49392 | 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 | |
---|---|---|---|---|---|---|---|---|
2023-06-26 | Fosaprepitant
172673-20-0
|
US $200.00 / kg | 1kg | 99% | 1000kg/Month | Hebei Mingeng Biotechnology Co., Ltd | ||
2023-04-11 | Fosaprepitant
172673-20-0
|
US $100.00 / KG | 25KG | 99% | 1000 Kilogram/Kilograms per Week | Shijiazhuang Gantuo Biotechnology Co., Ltd | ||
2021-08-31 | Fosaprepitant
172673-20-0
|
US $10.00 / KG | 1Kg/Bag | 99%min | 20000 | Wuhan Monad Medicine Tech Co.,LTD |
- Fosaprepitant
172673-20-0
- US $200.00 / kg
- 99%
- Hebei Mingeng Biotechnology Co., Ltd
- Fosaprepitant
172673-20-0
- US $100.00 / KG
- 99%
- Shijiazhuang Gantuo Biotechnology Co., Ltd
- Fosaprepitant
172673-20-0
- US $10.00 / KG
- 99%min
- Wuhan Monad Medicine Tech Co.,LTD