Aprepitant (MK-0869)

Catalog No. A10083

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.

  • Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
Catalog Num A10083
M. Wt 534.4
Formula C23H21F7N4O3
Purity >98%
Storage at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No. 170729-80-3
Synonyms MK0869, MK-869, L-754030, Emend
SMILES C[[email protected]](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[[email protected]@H]2[[email protected]@H](N(CCO2)CC3=NC(=O)NN3)C4=CC=C(C=C4)F

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.

Targets
Neurokinin-1 receptor (Cell-free assay)
0.1 nM
In vitro (25°C) DMSO 96 mg/mL (179.63 mM)
Water Insoluble
Ethanol 14 mg/mL (26.19 mM)
In vivo 5% DMSO+corn oil 12 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.