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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 |
|---|
| CRN04894
CRN04894 is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion. |
| BMS-470539
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. |
| PF-00446687
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. |
| BMS-470539 dihydrochloride
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. |
| Undecylenoyl phenylalanine
Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes. |
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