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THIQ
$61 – $935
Products Details
Product 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].
Web ID
– HY-10624
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C33H41ClN6O2
References
– [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.
CAS Number
– 312637-48-2
Molecular Weight
– 589.17
Compound Purity
– 98.48
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
Clinical Information
– No Development Reported
Research Area
– Metabolic Disease
Solubility
– DMSO : 250 mg/mL (ultrasonic)
Target
– Melanocortin Receptor
Isoform
– MC4R
Pathway
– GPCR/G Protein;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
