Description
| Description | Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), demonstrating EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) across species such as human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is applied in the study of skin pigmentation. |
| Targets&IC50 | MC4R (human):32.9 nM (Ki), MC3R (human):1420 nM (Ki), MC1R (cynomolgus monkey):3.91 nM (EC50), MC5R (human):486 nM (Ki), MC1R (mouse):1.14 nM (EC50), MC4R (human):79.6 nM (EC50), MC1R (rat):0.251 nM (EC50), MC1R (human):2.26 nM (Ki), MC1R (human):8.16 nM (EC50), MC2R (human):>10000 nM (EC50) |
| In vitro | Dersimelagon (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) enhances eumelanin synthesis in B16F1 cells in a concentration-dependent fashion, demonstrating an EC50 of 13 pM[1]. |
| In vivo | Dersimelagon (0.003, 0.03, 0.3, 3 mg/kg; p.o. for 6 days) induces coat colour darkening in Ay/a mice in 0.3 and 3 mg/kg[1]. |
| Synonyms | MT-7117 |
| Molecular Weight |
675.75 |
| Formula | C36H45F4N3O5 |
| CAS No. | 1835256-48-8 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 6.76 mg/mL (10 mM),
Sonication is recommended.
