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Aprepitant (MK-0869)

Catalog No.: A10083

neurokinin-1 receptor antagonist

Aprepitant (MK-0869)

Aprepitant (MK-0869) Chemical Structure

CAS NO. 170729-80-3

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.

Availability: In stock

Package Price Qty
2 mg
$30.00
5 mg
$50.00
10 mg
$60.00
25 mg
$70.00
10mM * 1mL in DMSO
$139.00
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  • 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

Biological Activity

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.

Catalog Num A10083
Actions Antagonist
CAS No. 170729-80-3
Formula C23H21F7N4O3
M. Wt 534.4
Purity >98%
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
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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