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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.
| Molecular Weight | 589.17 |
| CAS Number | 312637-48-2 |
| Solubility (25°C) | DMSO 150 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Melanocortin Receptor Products |
|---|
| α-MSH
α-MSH (α-Melanocyte-stimulating hormone) is a tridecapeptide, mostly produced by the cells in the brain, pituitary and circulation. |
| Melanotan I acetate
Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH). *This compound is unstable in solutions, freshly prepared is recommended. |
| Setmelanotide
Setmelanotide is a selective agonist of the MC4 receptor, with EC50 values of 0.27 nM and 0.28 nM for human and rat MC4R, respectively. |
| Bremelanotide Acetate
Bremelanotide Acetate (PT-141 Acetate) is a peptide containing seven amino acids and is also a macrocyclic compound. In addition, Bremelanotide Acetate is an agonist of the melanocortin 4 receptor (MC4R). |
| JNJ-10229570
JNJ-10229570 (UNII-N9IX402L35) is is a novel MC1R and MC5R antagonist, which inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R with IC50 values of 270 nM and 200 nM, respectively. |
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