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).
Technical Data
| M. Wt | 625.35 |
| Formula | C25H29BrF3N5O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 510732-84-0 |
| PubChem ID | 11479128 |
| InChI Key | BPGUWYBAINNZQH-UHFFFAOYSA-N |
| Smiles | BrC(C=C4)=CC(OC(F)(F)F)=C4CCN[C@@H](CC3)CC[C@@H]3NC2=NC1=CC=CC=C1C(N(C)C)=N2.Cl.Cl |
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
References
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 PMID:
Dyck et al (2005) Small molecule melanin-concentrating hormone receptor 1 (MCH1R) antagonists as anxiolytic and antidepressive agents. Drug Dev.Res. 65 291 PMID:
Keywords: ATC 0065, supplier, potent, selective, MCH, MCHR, MCH1R, MCHR1, antagonists, melanin, concentrating, hormone, receptors, serotonin, 5HT, ATC0065, Melanin-concentrating, Hormone, Receptors, Melanin-concentrating, Hormone, Receptors, Tocris Bioscience
