Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.
|Neurokinin-1 receptor (Cell-free assay)|
|In vitro (25°C)||DMSO||107 mg/mL (200.21 mM)|
|Water||<1 mg/mL (<1 mM)|
|Ethanol||15 mg/mL (28.06 mM)|
|In vivo||30% PEG400/0.5% Tween80/5% propylene glycol||30 mg/mL|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||18.71 mL||93.56 mL||187.13 mL|
|0.5 mM||3.74 mL||18.71 mL||37.43 mL|
|1 mM||1.87 mL||9.36 mL||18.71 mL|
|5 mM||0.37 mL||1.87 mL||3.74 mL|
*The above data is based on the productmolecular weight 534.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|MECHANISM OF ACTION||Antagonist|
|Storage||at -20°C 3 years Powder|
|Synonyms||MK0869, MK-869, L-754030, Emend|