THIQ

THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM) . THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants[1][2].

Product Specifications

CAS Number

[312637-48-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Melanocortin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/thiq.html

Concentration

10mM

Purity

98.48

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

ClC1=CC=C(C=C1)C[C@@H](NC([C@@H]2NCC3=CC=CC=C3C2)=O)C(N4CCC(C5CCCCC5)(CN6C=NC=N6)CC4)=O

Molecular Formula

C33H41ClN6O2

Molecular Weight

589.17

Precautions

H302, H315, H319, H335

References & Citations

[1]Sebhat IK, et al. 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-ylmethyl) piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. J Med Chem. 2002 Oct 10;45 (21) :4589-93.|[2]Huang H, et al. A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retainedmelanocortin-4 receptor mutants. Int J Biol Sci. 2014 Jul 20;10 (8) :817-24.