312637-48-2|(R)-N-((R)-1-(4-((1H-1,2,4-Triazol-1-yl)methyl)-4-cyclohexylpiperidin-1-yl)-3-(4-chlorophenyl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide|CsnPharm

CAS No.: 312637-48-2

THIQ Catalog No. CSN27581

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 .

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靶点选择性

生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6973 mL
- 8.4865 mL
- 16.9730 mL
- 5 mM
- 0.3395 mL
- 1.6973 mL
- 3.3946 mL
- 10 mM
- 0.1697 mL
- 0.8487 mL
- 1.6973 mL

技术信息

CAS号

312637-48-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H41ClN6O2

运输

蓝冰

分子量

589.17

别名

溶解度

DMSO	240.0 mg/mL (407.4 mM) warming

动物实验配方

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