THIQ
THIQ Basic information
- Product Name:
- THIQ
- Synonyms:
-
- 3-IsoquinolinecarboxaMide, N-[(1R)-1-[(4-chlorophenyl)Methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylMethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-, (3R)-
- (3R)-N-[(1R)-1-[(4-Chlorophenyl)Methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylMethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxaMide
- THIQ
- N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-trazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide
- (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
- (3R)-N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidiny
- mutant,MC Receptor,inhibit,THIQ,melanocortin,affinity,activity,erectile,selective,eliciting,Melanocortin Receptor,Inhibitor
- (3R)-N-[(2R)-3-(4-chlorophenyl)-1-{4-cyclohexyl-4-[(1H-1,2,4-triazol-1-yl)methyl]piperidin-1-yl}-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
- CAS:
- 312637-48-2
- MF:
- C33H41ClN6O2
- MW:
- 589.17
- Mol File:
- 312637-48-2.mol
THIQ Chemical Properties
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 250 mg/mL (424.33 mM; Need ultrasonic)
- form
- Powder
- pka
- 13.82±0.20(Predicted)
- color
- White to off-white
THIQ Usage And Synthesis
Uses
Melanocortin 4 receptors play important roles in the regulation of energy homeostasis, eating behavior and sexual functions (1). (3R)-N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide is a potent and selective melanocortin 4 receptor agonist (2,3). It inhibits parasympathetic preganglionic neurons in the brainstem and regulates sympathetic and parasympathetic preganglionic neurons.
Biological Activity
Potent and selective melanocortin 4 (MC 4 ) receptor agonist (IC 50 values are 1.2, 761 and 2067 nM for human MC 4 , MC 3 and MC 1 receptors respectively). Enhances intracavernosal pressure and stimulates erectile activity in rats ex copula following systemic administration.
in vivo
THIQ (0.3-10 mg/kg; i.v.) dose-dependently increases erections (ED50=0.87 mg/kg) in sexually mature male Sprague Dawley rats. The maximal increase in the number of erections (60%) is detected at 5 mg/kg but was not significantly different from that produced by 1 mg/kg. THIQ (20 mg/kg; p.o.) also produces statistically significant increases in erectile responses with a mean increase of 31±4%[1].
?
THIQ treatment shows the t1/2 is 0.6 hours in Sprague-Dawley rats (1 mg/kg, i.v. and 10 mg/kg, p.o.)[1].
IC 50
MC4R
storage
Store at -20°C
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