THIQ

CAT: 0804-HY-10624-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10624-01Size:1 mg
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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].
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.
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

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