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Aprepitant (MK-0869)

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neurokinin-1 receptor antagonist

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Catalog No. A10083

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
Aprepitant 2mg A10083-2

Regular Price: $30.00

Special Price: $24.00

Aprepitant 5mg A10083-5

Regular Price: $50.00

Special Price: $40.00

Aprepitant 10mg A10083-10

Regular Price: $60.00

Special Price: $48.00

Aprepitant 25mg A10083-25

Regular Price: $70.00

Special Price: $56.00

Aprepitant (MK-0869) 10mM * 1mL in DMSO A10083-10mM-D

Regular Price: $139.00

Special Price: $111.20

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

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.

Aprepitant (MK-0869)

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Chemical Information

Catalog Num A10083
Actions Antagonist
M. Wt 534.4
Formula C23H21F7N4O3
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 170729-80-3
Synonyms MK0869, MK-869, L-754030, Emend
SMILES code 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
Chemical Name 5-([(2R,3S)-2-((R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy)-3-(4-fluorophenyl) morpholino]methyl)-1H-1,2,4-triazol-3(2H)-one

Biological Activity

Description

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

Solubility

Solubility (25°C) * In vitro 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.

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