Pricing Availability   Qty
Description: Potent long-acting hNK1 antagonist
Chemical Name: 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
Purity: ≥99% (HPLC)
Citations (1)
Reviews (1)
Literature (2)

Biological Activity for Aprepitant

Aprepitant is a potent long-acting hNK-1 antagonist, (IC50 = 0.09 nM and Kd = 19 pM). Inhibits induced foot-tapping in gerbils. CNS penetrant and orally bioavailable. Antiemetic.

Compound Libraries for Aprepitant

Aprepitant is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Aprepitant

M. Wt 534.43
Formula C23H21F7N4O3
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 170729-80-3
PubChem ID 6918365
Smiles C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)O[C@H]2OCCN([C@H]2C3=CC=C(C=C3)F)CC4=NNC(N4)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Aprepitant

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 53.44 100
ethanol 5.34 10

Preparing Stock Solutions for Aprepitant

The following data is based on the product molecular weight 534.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.36 mL 18.71 mL
5 mM 0.37 mL 1.87 mL 3.74 mL
10 mM 0.19 mL 0.94 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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References for Aprepitant

References are publications that support the biological activity of the product.

Hale 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 recepto J.Med.Chem. 41 4607 PMID: 9804700

If you know of a relevant reference for Aprepitant, please let us know.

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1 Citation for Aprepitant

Citations are publications that use Tocris products. Selected citations for Aprepitant include:

Veronica A et al (2022) Dopamine D2 receptors bidirectionally regulate striatal enkephalin expression: Implications for cocaine reward. Cell Rep 40 111440 PMID: 36170833

Do you know of a great paper that uses Aprepitant from Tocris? Please let us know.

Reviews for Aprepitant

Average Rating: 5 (Based on 1 Review.)

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Very good product.
By Anonymous on 11/19/2020
Assay Type: In Vivo
Species: Mouse

In vivo, solution formulation

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.