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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)
Biological Activity for Aprepitant
Aprepitant is a potent long-acting hNK-1 antagonist (IC50 = 0.09 nM and Kd = 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.
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 |
| InChI Key | ATALOFNDEOCMKK-OITMNORJSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for Aprepitant
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
Jin et al (2022) Aprepitant attenuates NLRC4-dependent neuronal pyroptosis via NK1R/PKCd pathway in a mouse model of intracerebral hemorrhage. J.Neuroinflammation 19 198 PMID: 35922848
Padmanaban et al (2024) Neuronal substance P drives metastasis through an extracellular RNA-TLR7 axis. Nature 633 207 PMID: 39112700
Yang et al (2022) Aprepitant inhibits JNK and p38/MAPK to attenuate inflammation and suppresses inflammatory pain. Front.Pharmacol. 12 811584 PMID: 35087409
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Keywords: Aprepitant, Aprepitant supplier, human, substance, P/neurokinin, 1, NK1, hNK1, antagonists, antagonism, tachykinin, receptors, P, SP, antiemetics, CNS, penetrant, orally, bioavailable, Receptor, 6486, Tocris Bioscience
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
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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
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