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Aprepitant

Aprepitant Structure
CAS No.
170729-80-3
Chemical Name:
Aprepitant
Synonyms
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
Molecular Formula:
C23H21F7N4O3
Molecular Weight:
534.43
MOL File:
170729-80-3.mol
Modify Date:
2024/10/31 18:15:48

Aprepitant Properties

Melting point 244-246°C
alpha D25 +69° (c = 1.00 in methanol)
Density 1.51±0.1 g/cm3(Predicted)
storage temp. Sealed in dry,2-8°C
solubility Soluble in DMSO (>25 mg/ml)
pka 8.06±0.20(Predicted)
form powder
color white to beige
optical activity [α]/D +61 to +71°, c = 1.0 in methanol
Stability 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 DataBase Reference 170729-80-3(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07,GHS08
Signal word  Warning
Hazard statements  H319-H351
Precautionary statements  P501-P202-P201-P264-P280-P308+P313-P337+P313-P305+P351+P338-P405
HS Code  2934990002
NFPA 704
0
2 0

Aprepitant price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) SML2215 Aprepitant ≥98% (HPLC) 170729-80-3 5MG ₹9331.15 2022-06-14 Buy
Sigma-Aldrich(India) SML2215 Aprepitant ≥98% (HPLC) 170729-80-3 25MG ₹20112.85 2022-06-14 Buy
TCI Chemicals (India) A3135 Aprepitant 170729-80-3 100MG ₹8000 2022-05-26 Buy
TCI Chemicals (India) A3135 Aprepitant 170729-80-3 500MG ₹15000 2022-05-26 Buy
Product number Packaging Price Buy
SML2215 5MG ₹9331.15 Buy
SML2215 25MG ₹20112.85 Buy
A3135 100MG ₹8000 Buy
A3135 500MG ₹15000 Buy

Aprepitant Chemical Properties,Uses,Production

Description

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.

Chemical Properties

Off-White to Light Yellow Cyrstalline Solid

Uses

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.

References

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 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 616)Suppliers
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ANWITA APIS +919000311012 Hyderabad, India 195 58 Inquiry
Varanous Labs Pvt Ltd +91-7036248882 +91-7036248882 Hyderabad, India 1537 58 Inquiry
USV Pvt Ltd +91-2267861111 +91-2225564048 Maharashtra, India 36 58 Inquiry
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Nosch Labs Pvt Ltd +91-4048557474 +91-9948222287 Hyderabad, India 58 58 Inquiry
Mehta API Pvt. Ltd. +91-9920552082 +91-9920552082 Maharashtra, India 33 58 Inquiry
Solara Active Pharma Sciences Ltd +91-8046632100 +91-7075706520 Bangalore, India 65 58 Inquiry

Aprepitant Spectrum

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