Aprepitant

Name: Aprepitant
Brand: Tocris Bioscience
SKU: 6486

Tocris Bioscience, part of Bio-Techne | Catalog # 6486

(1)

Citations (8)

COA / SDS

Potent long-acting hNK1 antagonist

Key Product Details

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%

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Technical Data
Citations / Reviews (1)

Biological Activity for Aprepitant

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 for Aprepitant

Formula	C₂₃H₂₁F₇N₄O₃
Storage	Store at -20°C
Purity	≥99%
CAS Number	170729-80-3

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 for Aprepitant

Solubility

Soluble Soluble to 100 mM in DMSO and to 10 mM in ethanol

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References for Aprepitant

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

Hale et al. 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., 1998;41:4607 PMID: 9804700

Aprepitant

Tocris Bioscience, part of Bio-Techne | Catalog # 6486

Key Product Details

Biological Activity for Aprepitant

Technical Data for Aprepitant

Solubility for Aprepitant

Dilution Calculator

Reconstitution Calculator

References for Aprepitant

Product Documents for Aprepitant

COA

Certificate of Analysis

SDS

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