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
Literature

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.

All Tocris products are intended for laboratory research use only.

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

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.7 mL 8.49 mL 16.97 mL
5 mM 0.34 mL 1.7 mL 3.39 mL
10 mM 0.17 mL 0.85 mL 1.7 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: THIQ, supplier, Potent, selective, MC4R, receptors, agonists, Melanocortin, Melanocortin, Receptors, Melanocortin, Receptors, 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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