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Description: Potent and selective MC4 receptor agonist
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
Purity: ≥95% (HPLC)
Biological Activity for THIQ
THIQ is a 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 for THIQ
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for THIQ
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.89 | 10 |
Preparing Stock Solutions for THIQ
The following data is based on the product molecular weight 589.17. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 16.97 mL | 84.87 mL | 169.73 mL |
| 0.5 mM | 3.39 mL | 16.97 mL | 33.95 mL |
| 1 mM | 1.7 mL | 8.49 mL | 16.97 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.39 mL |
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Product Datasheets for THIQ
References for THIQ
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for THIQ, please let us know.
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Keywords: THIQ, THIQ supplier, Potent, selective, MC4R, receptors, agonists, Melanocortin, Receptors, 3032, Tocris Bioscience
3 Citations for THIQ
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
Sohn et al (2013) Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons. Int J Biol Sci 152 612 PMID: 23374353
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
Do you know of a great paper that uses THIQ from Tocris? Please let us know.
Reviews for THIQ
Average Rating: 5 (Based on 1 Review.)
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THIQ treatment increase social interactions.
By
Anonymous on 01/11/2019
Assay Type: In Vivo
Species: Mouse
Recently, we demonstrated that the deletion of the NFKB1 gene, which encodes the p50 NF-kappa B subunit, causes impairment in social behaviours, with reductions in social interactions in mice. In this work, we tested the acute effects of THIQ, a selective melanocortin 4 receptor (MC4R) agonist. THIQ treatment increased social interactions both in wild type and p50-/- mice. In particular, after treatment with THIQ, p50-/- mice showed a prosocial behaviour analogous to that of basal WT mice.
Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.