Biological Activity
Potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 1.2, 761 and 2067 nM for human MC4, MC3 and MC1 receptors respectively). Enhances intracavernosal pressure and stimulates erectile activity in rats ex copula following systemic administration.
Technical Data
| M. Wt | 589.17 |
| Formula | C33H41ClN6O2 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 312637-48-2 |
| PubChem ID | 9938402 |
| InChI Key | HLCHESOMJVGDSJ-LOYHVIPDSA-N |
| Smiles | O=[C@@]([C@H](NC([C@H]5CC(C=CC=C6)=C6CN5)=O)CC4=CC=C(Cl)C=C4)N1CCC(CN2N=CN=C2)(C3CCCCC3)CC1 |
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.
Preparing Stock Solutions
The following data is based on the product molecular weight 589.17. 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 | 1.7 mL | 8.49 mL | 16.97 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.39 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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References
References are publications that support the products' biological activity.
Sebhat et al (2002) Design and pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-methyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective melanocorti J.Med.Chem. 45 4589 PMID: 12361385
Martin et al (2002) Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula. Eur.J.Pharmacol. 454 71 PMID: 12409007
Mutulis et al (2004) New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J.Med.Chem. 47 4613 PMID: 15317471
Keywords: THIQ, supplier, Potent, selective, MC4R, receptors, agonists, Melanocortin, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
