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THIQ

Cat. No. 3032

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Chemical Name: N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-trazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide

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

Solubility:

Soluble to 10 mM in water

Purity:

>95 %

Storage:

Store at -20°C

CAS No:

312637-48-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Martin et al (2002) Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula. Eur.J.Pharmacol. 454 71. PMID: 12409007.

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 melanocortin subtype-4 receptor agonist. J.Med.Chem. 45 4589. PMID: 12361385.

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.

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