Aprepitant

Biological Activity

Aprepitant is a potent long-acting hNK-1 antagonist (IC₅₀ = 0.09 nM and K_d = 19 pM) that inhibits the effect of substance P on NK-1 receptors. Inhibits metastasis and impairs tumor growth in patient derived xenografts and breast cancer cells. In an animal model of intracerebral hemorrhage, Aprepitant reduces neurological impairment, neuronal damage and neuronal death. Suppresses pain and inflammation induced by formalin. Inhibits induced foot-tapping in gerbils. CNS penetrant and orally bioavailable. Antiemetic.

Technical Data

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.

Background References

1. 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
   Hale et al.
   J.Med.Chem., 1998;41:4607

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