Cat. No. 3359
Chemical Name: N2-[cis-4-[[2-[4-Bromo-2-(trifluoro
Biological ActivityOrally active, potent and selective melanin-concentrating hormone receptor 1 (MCH1) antagonist (IC50 = 15.7 nM) that displays > 96-fold selectivity over MCH2. Exhibits antidepressant and anxiolytic activity in vivo. Also displays affinity for 5-HT1A and 5-HT2B receptors (IC50 values are 62.9 and 266 nM respectively).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Kanuma et al (2006) Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists. Bioorg.Med.Chem. 14 3307. PMID: 16434202.
Chaki et al (2005) Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: Nonpeptide and orally active melanin-concentrating hormone receptor 1 antagonists. J.Pharmacol.Exp.Ther. 313 832.
Dyck et al (2005) Small molecule melanin-concentrating hormone receptor 1 (MCH1R) antagonists as anxiolytic and antidepressive agents. Drug Dev.Res. 65 291.
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Keywords: ATC 0065, supplier, potent, selective, MCH, MCHR, MCH1R, MCHR1, antagonists, melanin, concentrating, hormone, receptors, serotonin, 5HT, ATC0065, Tocris Bioscience, Melanin-concentrating Hormone Receptor Antagonist products
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