| Description | THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively). |
| In vitro | THIQ，一种MC4R的小分子激动剂，影响了十种内源性保留的MC4R突变体在不同细胞系上的细胞表面表达和信号传导。在HEK293细胞中，THIQ提高了三种突变体（N62S、C84R、C271Y）的细胞表面表达，并使其中两种（N62S和C84R）的信号传导增强。此外，THIQ也增强了另外两种突变体（P78L和P260Q）的信号传导，但未提高它们在HEK293细胞中的细胞表面表达。在神经细胞中，THIQ表现出更强的效果，修正了七种突变体（N62S、I69R、P78L、C84R、W174C、P260Q和C271Y）的细胞表面表达和信号传导。 |
| Target activity | MC4R (human):1.2 nM , MC4R (rat):0.6 nM |
| molecular weight | 589.17 |
| Molecular formula | C33H41ClN6O2 |
| CAS | 312637-48-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 245 mg/mL (415.84 mM), Sonication is recommended. |
| References | 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. |
| Citations | 1. Zhang, Yan, et al. Structural insights into ligand recognition and activation of the melanocortin-4 receptor. Cell Research. 2021, 31(11): 1163-1175. |