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THIQ

Catalog No. T8485   CAS 312637-48-2

THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).

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THIQ Chemical Structure
THIQ, CAS 312637-48-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 67.00
5 mg In stock $ 98.00
10 mg In stock $ 189.00
25 mg In stock $ 393.00
50 mg In stock $ 596.00
100 mg In stock $ 893.00
1 mL * 10 mM (in DMSO) In stock $ 136.00
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Purity: 98.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).
Targets&IC50 hMC4R:1.2 nM , rMC4R:0.6 nM
In vitro THIQ,?a small molecule agonist of the MC4R, on the cell surface expression and signaling of ten intracellularly retained MC4R mutants using different cell lines.?THIQ increased the cell surface expression of three mutants (N62S, C84R, and C271Y) and two of them (N62S and C84R) had increased signaling in HEK293 cells.THIQ increased the signaling of two other mutants (P78L and P260Q) without increasing their cell surface expression in HEK293 cells.?In neuronal cells, THIQ exhibited a more potent effect, correcting the cell surface expression and signaling of seven mutants (N62S, I69R, P78L, C84R, W174C, P260Q, and C271Y).
Molecular Weight 589.17
Formula C33H41ClN6O2
CAS No. 312637-48-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 245 mg/ml(415.84 mM), sonification is recommended.

TargetMolReferences and Literature

1. 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. 2. Sun X , Liu M , Gao L , et al. A novel tetrahydroisoquinoline (THIQ) analogue induces mitochondria-dependent apoptosis[J]. European Journal of Medicinal Chemistry, 2018:S0223523418302526. 3. 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.

TargetMolCitations

1. Zhang, Yan, et al. Structural insights into ligand recognition and activation of the melanocortin-4 receptor. Cell Research. 2021, 31(11): 1163-1175.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library GPCR Compound Library Anti-Obesity Compound Library Neuronal Signaling Compound Library

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Keywords

THIQ 312637-48-2 GPCR/G Protein Neuroscience Melanocortin Receptor mutant MC Receptor inhibit melanocortin affinity activity erectile selective eliciting Inhibitor inhibitor

 

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