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Potent long-acting hNK-1 antagonist, (IC50 = 0.09 nM and Kd = 19 pM). Inhibits induced foot-tapping in gerbils. CNS penetrant and orally bioavailable. Antiemetic.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
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
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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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.