产品说明书

THIQ

Print
Chemical Structure| 312637-48-2 同义名 : -
CAS号 : 312637-48-2
货号 : A1167673
分子式 : C33H41ClN6O2
纯度 : 99%+
分子量 : 589.171
MDL号 : MFCD09970598
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(424.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The melanocortin receptors are a family of seven-transmembrane G-protein-coupled receptors. The melanocortin subtype-4 receptor (MC4R) is expressed in various regions of the brain, and playing an important role in feeding behavior. THIQ is a potent and selective agonist of 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[3]. THIQ (10 μM; 24 h) decreased the signal intensity of WT MC4R by ~50% whereas increased that of three mutants (N62S, C84R, and C271Y) in HEK293 cells[4]. In sexually mature male Sprague Dawley rats, THIQ (0.3-10 mg/kg; i.v.) dose-dependently increased erections with an ED50 of 0.87 mg/kg. THIQ (20 mg/kg; p.o.) also produced statistically significant increases in erectile responses with a mean increase of 31 ± 4%[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.49mL

1.70mL

0.85mL

16.97mL

3.39mL

1.70mL
参考文献

[1]Sebhat IK, et al. Design and pharmacology of N-

[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.

[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

[4]Huang H, et al. A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants. Int J Biol Sci. 2014 Jul 20;10(8):817-24