Chemical Name:N2-[cis-4-[[2-[4-Bromo-2-(trifluoromethoxy)phenyl]ethyl]amino]cyclohexyl]-N4,N4-dimethyl-2,4-quinazolinediamine dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Orally 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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
62.53
100
ethanol
62.53
100
Preparing Stock Solutions
The following data is based on the product molecular weight 625.35. 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.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.6 mL
8 mL
15.99 mL
5 mM
0.32 mL
1.6 mL
3.2 mL
10 mM
0.16 mL
0.8 mL
1.6 mL
50 mM
0.03 mL
0.16 mL
0.32 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Kanumaet al (2006) Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists. Bioorg.Med.Chem. 14 3307 PMID: 16434202
Chakiet 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 PMID:
Dycket al (2005) Small molecule melanin-concentrating hormone receptor 1 (MCH1R) antagonists as anxiolytic and antidepressive agents. Drug Dev.Res. 65 291 PMID: