Catalog Number: 3032
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. All Tocris products are intended for laboratory research use only.
Background References
  1. Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula.
    Martin et al.
    Eur.J.Pharmacol., 2002;454:71
  2. 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
    Sebhat et al.
    J.Med.Chem., 2002;45:4589
  3. New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ".
    Mutulis et al.
    J.Med.Chem., 2004;47:4613
Citations:

The citations listed below are publications that use Tocris products. Selected citations for THIQ include:

3 Citations: Showing 1 - 3
Filter your results:

  1. A neural basis for melanocortin-4 receptor-regulated appetite.
    Authors: Garfield Et al.
    Nat Neurosci 2015;18:863
  2. A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants.
    Authors: Huang and Tao
    Front Pharmacol 2014;10:817
  3. Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons.
    Authors: Sohn Et al.
    Int J Biol Sci 2013;152:612

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