Cat. No. 3032
Chemical Name: N-[(1R)-1-[(4-Chlorophenyl)methyl]-
Biological ActivityPotent 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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.
If you know of a relevant reference for THIQ please let us know.
Citations are publications that use Tocris products. Selected citations for THIQ include:
Garfield et al (2015) A neural basis for melanocortin-4 receptor-regulated appetite. Nat Neurosci 18 863. PMID: 25915476.
Huang and Tao (2014) A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants. Front Pharmacol 10 817. PMID: 25076858.
Sohn et al (2013) Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons. Int J Biol Sci 152 612. PMID: 23374353.
Do you know of a great paper that uses THIQ from Tocris? If so please let us know.
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Keywords: THIQ, supplier, Potent, selective, MC4R, receptors, agonists, Melanocortin, Tocris Bioscience, Melanocortin (MC) Receptor Agonist products
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