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Aprepitant

Chemical Structure : Aprepitant

CAS No.: 170729-80-3

Aprepitant (MK-0869;MK-869;L-754030)

Catalog No.: PC-42185Not For Human Use, Lab Use Only.

Aprepitant (MK-0869) is a potent, orally active, long-acting human NK-1 receptor (substance P receptor) antagonist with IC50 of 0.09 nM.

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Biological Activity

Aprepitant (MK-0869) is a potent, orally active, long-acting human NK-1 receptor (substance P receptor) antagonist with IC50 of 0.09 nM.
Aprepitant (MK-0869) blocks NK-1 agonist-induced foot tapping response in gerbils and shows antiemetic actions in the ferret against cisplatin challenge.
Aprepitant (MK-0869) has the potentiation for the treatment of peripheral pain, migraine, chemotherapy-induced emesis, and various psychiatric disorders.

Physicochemical Properties

M.Wt 534.4266
Formula C23H21F7N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3H-1,2,4-Triazol-3-one, 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-

References

1. Kramer MS, et al. Science. 1998 Sep 11;281(5383):1640-5.

2. Hale JJ, et al. J Med Chem. 1998 Nov 5;41(23):4607-14.

3. Tattersall FD, et al. Neuropharmacology. 2000 Feb 14;39(4):652-63.

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