THIQ

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Cat.No. 3032 - THIQ | C33H41ClN6O2 | CAS No. 312637-48-2
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)
Datasheet
Citations (3)
Reviews (1)
Literature (3)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 5.89 10

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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

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


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Reviews for THIQ

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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.


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