Aprepitant
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- CAS-Nr.
- 170729-80-3
- Englisch Name:
- Aprepitant
- Synonyma:
- 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one;Emend;Aprepitan;5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one;CS-274;MK-0869;ONO 7436;aprepitant;Aprepirant;Fushapitan
- CBNumber:
- CB7500857
- Summenformel:
- C23H21F7N4O3
- Molgewicht:
- 534.43
- MOL-Datei:
- 170729-80-3.mol
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Aprepitant Eigenschaften
- Schmelzpunkt:
- 244-246°C
- alpha
- D25 +69° (c = 1.00 in methanol)
- Dichte
- 1.51±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,2-8°C
- Löslichkeit
- Soluble in DMSO (>25 mg/ml)
- pka
- 8.06±0.20(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
- Optische Aktivität
- [α]/D +61 to +71°, c = 1.0 in methanol
- Stabilität:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- CAS Datenbank
- 170729-80-3(CAS DataBase Reference)
Aprepitant Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Aprepitant is an antiemetic chemical compound that belongs to “substance P” antagonists (SPA) with its effect being blocking the neurokinin 1(Nk1) receptor. It is used for the prevention of acute and delayedchemotherapy-induced nausea and vomiting(CINV) and for prevention ofpostoperative nausea and vomiting. It can also be used for the treatment of cyclic vomiting syndrome and late-stage chemotherapy induced vomiting occurring during cancer treatment. Aprepitant alleviates the case of vomiting in patients through balking the signals released by Nk1 receptors. Nk1 is a G-protein-coupled receptor with its ligand being substance P (SP). The high concentration of SP is required for the vomiting reflex. Aprepitant blocks the process of SP-NK1 signaling in activating the vomiting reflex.
Chemische Eigenschaften
Off-White to Light Yellow Cyrstalline Solid
Verwenden
A novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes indicate that Aprepitant is metabolised primarily by CYP3A4 with minor metabolism by CYP1A2 and
CYP2C19, and no metabolism by CYP2D6, CYP2C9, or CYP2E1. Antiemetic.
Definition
ChEBI: A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/
eurokinin 1 (NK1) receptors.
Einzelnachweise
Curran, Monique P., and D. M. Robinson. "Aprepitant."Drugs69.13(2009):1853-1878.
Sant P. Chawla M.D. † ‡, et al. "Establishing the dose of the oral NK 1, antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting." Cancer 97.9(2003):2290-2300.
Warr, D. G., et al. "Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy." Journal of Clinical Oncology Official Journal of the American Society of Clinical Oncology23.12(2005):2822-30.
https://en.wikipedia.org/wiki/Aprepitant
Aprepitant Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Aprepitant Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 610)Lieferanten
170729-80-3()Verwandte Suche:
- MK-0869
- 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,
- 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one, Emend
- Aprepitant(MK-0869)
- ONO 7436
- 5-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)Morpholino)Methyl)-1H-1,2,4-triazol-3(2H)-one
- Aprepirant
- aprepitant
- 5-[2(R)-[1(R)-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-ylmethyl]-3,4-dihydro-2H-1,2,4-triazol-3-one MK0869 Aprepitant
- mk 0869
Aprepitant
- Aprepitant, >=99%
- 3-(((2R,3S)-2-((R)-1-(3,5-Bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)meth
- 3-(((2R,3S)-2-((R)-1 -(3,5-bis(trifluoromethyl)phenyl) ethoxy)-3-(4-fluorophenyl)morpholino)methyl)- 1H-1,2,4-triazol-5(4H)-one (Aprepitant)
- 5-[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)morpholin-4-ylmethyl]-3,4-dihydro-2h-1,2,4-triazol-3-one
- CS-274
- Aprepitant (MK-0869, L-754030)
- Fosaprepitant Impurity 8(Aprepitant)
- Fushapitan
- Aprepitant CRS
- (1R,2R,3S)-Aprepitant
- Aprepitant USP/EP/BP
- 5-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
- Aprepitant (Y0001825)
- AprepitantQ: What is
Aprepitant Q: What is the CAS Number of
Aprepitant Q: What is the storage condition of
Aprepitant Q: What are the applications of
Aprepitant
- Aprepitant (1041904)
- tetrapotassium salt
- 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one
- Emend
- 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one
- Aprepitan
- His minions pyrazole temple
- c . (6a R)-9-[7,8-d i d e h yd ro-4,5α-e poxy-3-h yd roxy-17-me th ylmorph i na n-6α-yl]-6-me th yl-5,6,6a ,7-te tra h yd ro-4h -d i b e nzo[d e ,g ]qui noli ne -10,11-d i ol (morph i ne -a pomorph i ne d i me r).
- 5-[2(R)-[1(R)-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-ylmethyl]-3,4-dihydro-2H-1,2,4-triazol-3-one
- 5-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-2,3-dihydro-1H-1,2,4-triazol-3-one
- 170729-80-3
- C23H21F7N4O3
- Inhibitors
- Aprepitant
- Pharmaceutical intermediate
- Chiral Reagents
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- API
- 170729-80-3
