1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor
  3. THIQ

THIQ 

Cat. No.: HY-10624 Purity: 98.48%
Handling Instructions

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.

For research use only. We do not sell to patients.

THIQ Chemical Structure

THIQ Chemical Structure

CAS No. : 312637-48-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 167 In-stock
Estimated Time of Arrival: December 31
5 mg USD 129 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 935 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

In Vitro

THIQ maintains low potency at human MC1R, MC3R and MC5R with IC50s of 2067, 761, 326 nM and EC50s of 2850, 2487, 737 nM, resepectively. THIQ maintains low potency at rat MC3R and MC5R with IC50s 1883 and 1575 nM, and EC50s of 1325 and >3000 nM, respectively[1].
THIQ (10 μM; 24 hours) decreases the signal intensity of WT MC4R by approximately 50% whereas increases that of three mutants (N62S, C84R, and C271Y) in HEK293 cells[2].

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].

Molecular Weight

589.17

Formula

C₃₃H₄₁ClN₆O₂

CAS No.

312637-48-2

SMILES

ClC1=CC=C(C=C1)C[[email protected]@H](NC([[email protected]@H]2NCC3=CC=CC=C3C2)=O)C(N4CCC(C5CCCCC5)(CN6C=NC=N6)CC4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (424.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

THIQMelanocortin ReceptorMC ReceptormelanocortinselectiveelicitingerectileactivitymutantaffinityInhibitorinhibitorinhibit

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THIQ
Cat. No.:
HY-10624
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