THIQ

• Description :

  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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  MC4R

• CAS Number :

  [312637-48-2]