AprepitantA selective neurokinin-1 (NK-1) receptor antagonist

Aprepitant (CAS 170729-80-3)

Aprepitant | CAS 170729-80-3 is rated 5.0 out of 5 by 1.
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Synonym: 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; MK-0869
Application: A selective neurokinin-1 (NK-1) receptor antagonist
CAS Number: 170729-80-3
Purity: ≥99%
Molecular Weight: 534.43
Molecular Formula: C23H21F7N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Aprepitant is a novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes show that it is metabolized primarily by CYP3A4 with minor metabolism by CYP2C19 and CYP1A2.


References

1. Hale, J J., et al., 1998. Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. Journal of medicinal chemistry. 41(23): 4607-14. PMID: 9804700
2. Campos, D., et al., 2001. Prevention of cisplatin-induced emesis by the oral neurokinin-1 antagonist, MK-869, in combination with granisetron and dexamethasone or with dexamethasone alone. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 19(6): 1759-67. PMID: 11251007
3. Van Belle, Simon., et al., 2002. Prevention of cisplatin-induced acute and delayed emesis by the selective neurokinin-1 antagonists, L-758,298 and MK-869. Cancer. 94(11): 3032-41. PMID: 12115394
4. Majumdar, Anup K., et al., 2006. Pharmacokinetics of aprepitant after single and multiple oral doses in healthy volunteers. Journal of clinical pharmacology. 46(3): 291-300. PMID: 16490805

Physical State :
Solid
Storage :
Store at -20° C
Melting Point :
242-250° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
151165
SMILES :
C[C@@H](O[C@H]1OCCN(CC2=NNC(=O)N2)[C@H]1C1=CC=C(F)C=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F

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Certificate of Analysis

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Aprepitant  Product Citations

See how others have used Aprepitant. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 27609608  Bayati, S. et al. 2016. Eur. J. Pharmacol. 791: 274-283.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Van Belle et al Van Belle et al. (PubMed ID 12115394) found that dual therapy with dexamethasone and aprepitant was superior to ondansetron with dexamethasone for the control of delayed emesis. -SCBT Publication Review
Date published: 2015-01-07
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