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Potent, selective melanin-concentrating hormone receptor 1 (MCH1R) antagonist (IC50= 5.6 nM in hMCH1R-expressing CHO cells). Displays selectivity for MCH1R over MCH2R (IC50 = > 10 μM). Decreases body weight in a mouse model of diet-induced obesity. Brain penetrant; orally active.
|Storage||Store at RT|
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 408.47. 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||2.45 mL||12.24 mL||24.48 mL|
|5 mM||0.49 mL||2.45 mL||4.9 mL|
|10 mM||0.24 mL||1.22 mL||2.45 mL|
|50 mM||0.05 mL||0.24 mL||0.49 mL|
References are publications that support the biological activity of the product.
Haga et al (2011) Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists. Bioorg.Med.Chem. 19 883 PMID: 21190859
Ito et al (2009) Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice. Eur.J.Pharmacol. 624 77 PMID: 19836369
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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!
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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.